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CURRICULUM VITAE Stephen P. Arneric, Ph.D. Home : 231-861-7382 Mobile: 231-740-0268 Email: [email protected] 2913 S. Timber Dunes Drive Shelby, MI, 49455 Professional Profile A pharmaceutical scientist and leader with a proven track record to deliver differentiated therapeutics. Experience spanning more than 25+ years of large pharma (Abbott, Lilly, Pharmacia, & Pfizer), biotechnology (DuPont Pharmaceuticals, Neuromed Pharmaceuticals), and academic service (University of Iowa, Cornell Medical College, Southern Illinois University School of Medicine) that resulted in 30+ drug candidates entering into clinical development to treat pain, neurological, psychiatric and urological disorders. Demonstrated ability to lead complex cross-functional matrix organizations of 100+ staff, and effectively manage $20MM budgets within target. Ph3 or Launched Product Development experience with the following: Exalgo™(Oros-hydromorphone for OA & CLBP), Esreboxetine (DPNP), Dynastat™(acute pain), Lyrica™(neuropathic pain), Cymbalta™ (musculoskeletal pain, fibromyalgia, DPNP), Mirapex™(Parkinson’s Disease, RLS) and Detrol™(overactive bladder). A leader that leverages global alliances and cross-organizational strengths to maximize organizational efficiencies (Merck, Recordati, Covance, NeuroSearch, RaQualia, Jubilant, Noxxon, Arteus, PsychoGenics, AnaBios, Chorus, Scripps, Univ of Pittsburgh, University of Colorado, University of Geneva, ORCATECH, Univ. of Arizona, Univ. of British Columbia, etc.). An medical educator experienced teaching medical students, graduate students, and neuroscience medical liaisons currently Adjunct Professor of Pharmacology, SIU School of Medicine. An accomplished author with 145 peer-reviewed articles, 190 abstracts, 17 chapters, 1 book, numerous IND submissions, as well as a co-inventor of 15 patents. A professional with a high aptitude for strategic, critical and tactical thinking that evaluates both scientific & business conditions resulting in effective solutions to challenges across diverse functions within the organization. Professional Expertise Drug Discovery & Development Leadership in complex matrix organizations Translational Sciences Pharmacology Novel drug/device combos Medical Education Global Initiatives Alliance & program management Establishing, growing & leading new organizations Opportunity Identification & Business Development Creative deal structures

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CURRICULUM VITAE

Stephen P. Arneric, Ph.D.

Home : 231-861-7382 Mobile: 231-740-0268

Email: [email protected]

2913 S. Timber Dunes Drive Shelby, MI, 49455

Professional Profile

A pharmaceutical scientist and leader with a proven track record to deliver differentiated therapeutics. Experience spanning more than 25+ years of large pharma (Abbott, Lilly, Pharmacia, & Pfizer), biotechnology (DuPont Pharmaceuticals, Neuromed Pharmaceuticals), and academic service (University of Iowa, Cornell Medical College, Southern Illinois University School of Medicine) that resulted in 30+ drug candidates entering into clinical development to treat pain, neurological, psychiatric and urological disorders. Demonstrated ability to lead complex cross-functional matrix organizations of 100+ staff, and effectively manage $20MM budgets within target. Ph3 or Launched Product Development experience with the following: Exalgo™(Oros-hydromorphone for OA & CLBP), Esreboxetine (DPNP), Dynastat™(acute pain), Lyrica™(neuropathic pain), Cymbalta™ (musculoskeletal pain, fibromyalgia, DPNP), Mirapex™(Parkinson’s Disease, RLS) and Detrol™(overactive bladder). A leader that leverages global alliances and cross-organizational strengths to maximize organizational efficiencies (Merck, Recordati, Covance, NeuroSearch, RaQualia, Jubilant, Noxxon, Arteus, PsychoGenics, AnaBios, Chorus, Scripps, Univ of Pittsburgh, University of Colorado, University of Geneva, ORCATECH, Univ. of Arizona, Univ. of British Columbia, etc.). An medical educator experienced teaching medical students, graduate students, and neuroscience medical liaisons – currently Adjunct Professor of Pharmacology, SIU School of Medicine. An accomplished author with 145 peer-reviewed articles, 190 abstracts, 17 chapters, 1 book, numerous IND submissions, as well as a co-inventor of 15 patents. A professional with a high aptitude for strategic, critical and tactical thinking that evaluates both scientific & business conditions resulting in effective solutions to challenges across diverse functions within the organization.

Professional Expertise

Drug Discovery & Development

Leadership in complex matrix organizations

Translational Sciences

Pharmacology

Novel drug/device combos

Medical Education

Global Initiatives

Alliance & program management

Establishing, growing & leading new organizations

Opportunity Identification & Business Development

Creative deal structures

Stephen P. Arneric, Ph.D. – April, 2015 2

PROFESSIONAL EXPERIENCE

Independent Consultant February 2015 - present Eli Lilly & Company January 2012- Dec. 2014 Indianapolis, IN Senior Research Fellow, Neuroscience Discovery Led projects related to the discovery and development of pain therapeutics across small molecule and biologics approaches. Direct line management responsibility of 1 scientist. Primary responsibility of in-licensing evaluations for the Pain Portfolio. Research Steering Committee member responsibilities for Jubilant (Bangalore, India), Arteus (mAb for Pain) and Covance (Greenfield, IN). Reporting to: Ronald B Demattos, Ph.D., CSO, Neuroscience Biologics, Indianapolis Neuroscience Site Head (2014-present); Olof Larsson, D.D.S., Ph.D., CSO, Pain & Migraine Drug Hunting Team, Neuroscience Discovery Research(2012-2014). Eli Lilly & Company (2008- 2011) Indianapolis, IN Chief Scientific Officer, Pain & Migraine Drug Hunting Teams Led the discovery and development of pain therapeutics across small molecule and biologics approaches which led to the first CGRP Ab to enter clinical development for migraine. Established Lilly as a player in ion channel pain therapeutics. Direct line management responsibility of 33 scientists at the Indianapolis (US) and Erl Wood (UK) research sites. Matrix leadership of 130+ scientists and support staff including molecular pharmacologists, electrophysiologists, behavioral pharmacologists, ADME, CMC, legal, regulatory, business development, new product planning, licensing, medical liaisons, and toxicology expertise. Research Steering Committee member responsibilities for Noxxon Pharma (Berlin, Germany), NeuroSearch (Copenhagen, Denmark) collaborations, RaQualia (Nagoya, Japan), Jubilant (Bangalore, India), Arteus and Covance (Greenfield, IN). Reported to: David Bredt, M.D., PhD (2008-2010); Christer Nordstedt, M.D., Ph.D., VP Neuroscience Discovery Research & Clinical Development, (2008- 2011). Neuromed Pharmaceuticals (2006- 2008) Vancouver, BC, Canada

VP, Research & Preclinical Development. Led the discovery and development of therapeutics targeting modulation of calcium channels. The N-Type calcium channel program was partnered with Merck for the treatment of pain and other CNS disorders. The T-type platform was a series of programs targeting calcium channels involved in a number of pain, neurologic, psychiatric and cardiovascular disorders, and is the main focus of Neuromed’s intenal discovery efforts. Led 50 scientists including molecular pharmacologists, electrophysiologists, behavioral pharmacologists, ADME, CMC and toxicology experts. Managed $20MM budget to target. Leader of: scientific direction; creation and management of milestones, impact goals and long range plans; hiring of staff and reallocation of project resources; mentoring career development of junior staff; initiating and maintaining coordination of efforts related to clinical research, marketing; discovery input to clinical trial design and clinical research interfacing; initiating and maintaining outside contract research; and licensing. Reported to Christopher Gallen, M.D., CEO and President, (2006-2008)

Stephen P. Arneric, Ph.D. – April, 2015 3

PFIZER, INC. (2003-2006) Psychotherapeutics Ann Arbor, MI

Senior Director & Head of CNS Biology at the Ann Arbor Laboratories. A variety of molecular targets including GPCRs and ion channels were targeted for the potential treatment of depression, anxiety, bipolar disorders, pain, schizophrenia, smoking cessation, substance abuse, and attention deficit hyperactivity disorder.

Drove the delivery of 14 compounds into development from 2003-2006. Contributed to the late stage development activities for Reboxetine and Pregabalin.

Led 60 scientists including molecular pharmacologists, electrophysiologists and behavioral pharmacologists.

Task Force member of 3 Global Initiatives: Strategic Plan for Depression; Strategic Plan for Cognitive Therapies; Tranlational Pharmacology Imperatives to Reduce Attrition

Leader of: scientific direction; creation and management of milestones, impact goals and long range plans; hiring of staff and reallocation of project resources; initiating and maintaining coordination of efforts related to clinical research, marketing; discovery input to clinical trial design and clinical research interfacing; initiating and maintaining outside contract research.

PHARMACIA (2000-2003) Neuroscience Kalamazoo, MI Senior Director of Neurobiology and CNS Discovery. A variety of molecular targets including GPCRs and ion channels are being targeted for the potential treatment of Alzheimer’s disease, Parkinson’s disease, depression, anxiety, neuropathic pain, migraine, schizophrenia, obesity, smoking cessation, attention deficit hyperactivity disorder and urology disorders.

Delivered 6 compounds into development from 2001-2002.

Contributed to late stage (Phase III & IV) development activities for Reboxetine, Xanax™, Mirapex™, Deramciclane, and Dynastat.

Led the Discovery interface of the Joint Research Committee for the Pharmacia/Recordati alliance for a Urology product.

Led scientific direction of 55 scientists including biochemical pharmacologists, electrophysiologists and behavioral pharmacologists.

Chair of CNS Core Team that governed: the scientific direction; creation and management of milestones, impact goals and long range plans; hiring of staff and reallocation of project resources; initiating and maintaining coordination of efforts related to clinical research, marketing; key member of CNS licensing team; discovery input to clinical trial design and clinical research interfacing; initiating and maintaining outside contract research. Reported to: David W. Robertson, Ph.D., Vice President, CNS Research (2000-2001; Donald E. Frail, Ph.D., Vice President, CNS Research (2001-2003)

DUPONT PHARMACEUTICALS (1998-2000) Neuroscience Wilmington, DE Senior Director of CNS Pharmacology for Secretase Program, CRF Program, 5-HT2c and ADHD Programs. These programs targeted the therapeutic areas of Alzheimer’s disease, depression, anxiety, obesity and attention deficit hyperactivity disorders. Also responsible for the behavioral evaluation of compounds for the obesity and antipsychotic programs.

Stephen P. Arneric, Ph.D. – April, 2015 4

ABBOTT LABORATORIES (1989-1998) NEUROLOGICAL and UROLOGICAL RESEARCH Abbott Park, IL Group Leader; Acting Project Leader for Cognitive Function Group (D-47W) -

Led 24 scientists (8 Ph.D.; 16 Associates) including chemists, molecular biologists, biochemists, pharmacologists and behavioral pharmacologists

Led the molecular biology of neurotrophic factor efforts (NGF, NGF receptor and BDNF) including screening and secondary biochemical and behavioral testing for small molecule mimetics

Authored NIA Drug Discovery Effort Proposal for AD: "NGF Receptor Proteases in Neural Degeneration"

Established nicotinic acetylcholine ligand approach to enhance cognitive performance

Project Leader for Cholinergic Channel Modulators (D-47W) -

Led 32 scientists (13 Ph.D.; 19 Associates) including chemists, molecular biologists, biochemical pharmacologists, electrophysiologists and behavioral pharmacologists. Managed to target > $6 million/yr budget.

Directed biology and chemistry supporting the Phase II development compound, ABT-418, a transdermal formulation for the potential treatment of Alzheimer's disease (AD). Approved for development 9/92. Human trials initiated 7/93; design and execution of preclinical pharmacology leading to IND filings for AD (10/93) and smoking cessation (12/93); Phase II efficacy demonstrated for smoking cessation, 3Q '94; Phase II AD efficacy trials discontinued due to lack of sufficient efficacy, 12/95; Phase II Attention deficit hyperactivity disorder trial initiated 3Q '96.

Responsible for initiating and coordinating efforts to develop what may be the first NCE to be developed specifically as a transdermal formulation (6/93).

Directed efforts to clone human neuronal nicotinic acetylcholine receptors (nAChRs). Was the first group to stably transfect the two putative major subtypes of nAChRs in

human brain (i.e. and ).

Initiated first PPD analgesia discovery program; Discovered and characterized ABT-594, the first orally effective, broad spectrum analgesic compound for acute and neuropathic pain, that mediates analgesia via cholinergic channel modulation.

Director for Cholinergic Channel Modulators (D-47W) and Purinergic Modulation (D- 4PM) Programs. These programs were covering the therapeutic areas of acute and neuropathic pain.

Led/managed 63 scientists (25 Ph.D.; 38 Associates) including chemists, molecular biologists, biochemical pharmacologists, electrophysiologists and behavioral pharmacologists. Budgetary responsibility of > $12 million/yr.

Responsible for: scientific direction; creation and management of milestones, impact

goals and long range plans; hiring of staff and reallocation of project resources; initiating and maintaining divisional coordination of efforts related to clinical research, marketing, diagnostics, hospital products and chemical products divisions; discovery input to clinical trial design and venture clinical research interfacing; initiating and maintaining outside contract research totaling $500,000. Reported to: Michael Williams, Ph.D., D.Sc., Div. Vice President, Neurological and Urological Diseases Discovery Research

Stephen P. Arneric, Ph.D. – April, 2015 5

IND SUBMISSIONS (directly led preclinical submission)

1. ABT-418 (A-81418)[(S)-3-methyl-5-(1-methyl-2-pyrrolidinyl) isoxazole hydrochloride]: A Novel Cholinergic Channel Activator for the Treatment of Alzheimer's Disease , Submitted to FDA in October, 1993.

2. ABT-418 (A-81418)[(S)-3-methyl-5-(1-methyl-2-pyrrolidinyl) isoxazole hydrochloride]: A Novel Cholinergic Channel Activator for the Treatment of Smoking Cessation, Submitted to FDA in December, 1993.

3. ABT-594 (A-165594) [5-((2R)-azetidinylmethoxy)-2-chloropyridine] : A Novel Cholineric Channel Modulator for General Pain Management, Submitted to FDA in February, 1998.

4. Was responsible for IND submissions of more than several dozen other compounds after leaving Abbott.

ACADEMIC APPOINTMENTS

Jan. 2007- Honorary Research Associate, Michael Smith Labs present University of British Columbia July 1996- Adjunct Professor, Department of Pharmacology, present Southern Illinois University School of Medicine, Springfield, IL July 1992- Adjunct Associate Professor, Department of Pharmacology, 1996 Southern Illinois University School of Medicine, Springfield, IL

1989-1992 Adjunct Assistant Professor, Department of Pharmacology, Southern Illinois University School of Medicine, Springfield, IL 1986-1989 Assistant Professor, Department of Pharmacology Southern Illinois University School of Medicine, Springfield, IL 1985-1986 Assistant Professor, Laboratory of Neurobiology, Department of Neurology, Cornell University Medical College, New York NY 1984-1985 Instructor, Laboratory of Neurobiology Department of Neurology, Cornell University Medical College, York, NY 1983-1985 Merck Foundation Postdoctoral Training Fellowship Laboratory of Neurobiology, Department of Neurology Cornell University Medical College, New York, NY 1979-1983 NIH Predoctoral Trainee, Department of Pharmacology, University of Iowa, Iowa City, IA 1979 Research Assistant, Dept. of Pharmacology, Michigan State University, East Lansing, MI 1978 Student Chemist, Biochemistry Laboratory Dow Chemical Co., Midland, MI 1977-1979 Undergraduate Teaching Assistantship, Lyman Briggs College, Michigan State University, East Lansing, MI 1977 Student Chemist, Toxicology Laboratory Dow Chemical Co., Midland, MI

Stephen P. Arneric, Ph.D. – April, 2015 6

EDUCATION

B.S. 1979 Michigan State University, East Lansing, MI

Physical Science (Lyman Briggs College ) Ph.D. 1983 University of Iowa, Iowa City, IA

Pharmacology Dissertation: "Dopamine analog-induced hyperglycemia in the rat: Investigations determining the role of the endocrine pancreas and the autonomic nervous system". Dissertation Advisor: John P. Long, Ph.D.

Postdoc. 1983-85 Cornell University Medical College New York, NY (Neurobiology/Cerebral Circulation)

Postdoctoral Advisor: Donald J. Reis, M.D. Postgraduate courses:

Molecular Approaches for Neurosciences: June, 1996 Measuring Gene Expression Promega, Madison, WI (Five day lab/lecture course) Management Courses Management Through Goals December 1991 Abbott Laboratories (Two day course) Technical Leadership November 1990 Mohr Development (Five day course) Leadership Intensive September 2001 Pharmacia Corporation (Three day course) Essentials for Pfizer Managers January 2004 Pfizer Inc (Three day course)

AWARDS AND HONORS

1996 PPD Chairman's Award, Abbott Laboratories 1995-1998 Research Fellow, Volwiler Fellow, Abbott Laboratories 1993 PPD Chairman's Award, Abbott Laboratories 1989 Recipient of the A. Paul Naney Research Award from the Illinois Affiliate of the

American Heart Assoc. 1983-1985 Postdoctoral Training Fellowship from the Merck Foundation 1982 Individual National Research Service Award, National Institute of Health (MH 08857) 1979; 1983 Graduated cum laude

Stephen P. Arneric, Ph.D. – April, 2015 7

PROFESSIONAL ORGANIZATIONS American Chemical Society American College of Neuropsychopharmacology, Member American Society for Pharmacology and Experimental Therapeutics American Society for Experimental NeuroTherapeutics, Inc. International Society for Cerebral Blood Flow and Metabolism International Society for Autonomic Neuroscience, Charter Member Society for Neuroscience Society for Research on Nicotine and Tobacco, Charter Member

PROFESSIONAL ACTIVITIES

2010-2014 Lilly Neuroscience Strategy Team 2010-2012 Lilly Chair, RaQualia Joint Steering Committee 2010-2013 Lilly Jubilant, Target Selection Steering Committee 2009-2010 Lilly Noxxon Joint Research Steering Committee 2009-2012 Lilly Neurosearch Joint Research Steering Committee 2009-2010 Lilly Target Development Committee 2007-2008 Neuromed Full Development Committee 2007-2008 Neuromed Early Development Committee 2004-2006 Pfizer Inc Global Translational Pharmacology Team 2004-2006 Pfizer Inc Ann Arbor Translational Pharmacology Team 2004-2006 Pfizer Inc CNS Disease Area Working Group 2003-2006 Pfizer Inc Biology Leadership Team 2003-2006 Pfizer, Inc Discovery Management Forum 2003-2006 Pfizer Inc CNS Therapeutic Areas Goals Team 2003-2006 Pfizer Inc Chair, CNS Pharmacology Operations Team 2003-2006t Pfizer Inc CNS Core Team 2002-2003 Pharmacia Chair, CNS Therapeutic Areas Core Team 2001-2003 Pharmacia Paracoxib BDT 2001-2003 Pharmacia Reboxetine Development Team 2001-2003 Pharmacia/Recordati Joint Research Committee 2000-2003 Pharmacia CNS Research Therapeutic Area Team 2000-2003 Pharmacia Pain Working Group 1998-2000 DuPont Research Management Council 1996-1998 ABBOTT Discovery Research Council 1995-1998 ABBOTT Neuroscience Technology Assessment Team 1995-1998 ABBOTT High Throughput Screening Restrictions Committee 1992-1998 ABBOTT Neuroscience Strategic Planning Team 1992-1998 ABBOTT Action Planning Committee for Cholinergic Channel Modulation 1991-1992 ABBOTT Behavioral Neuroscience Steering Committee 1990-1991 ABBOTT Neuroscience Long Range Planning Committee 1990-1991 ABBOTT Action Planning Committee for Cognitive Function Project 1989-1990 American Heart Assoc./Ill. Affl.-Research Policy & Allocations Committee 1988-1990 SIU Director, Pharmacology Graduate Program 1988-1990 SIU Laboratory Animal Care and Use Committee 1988-1990 American Heart Assoc./Ill. Affl.- Board of Directors 1987-1989 SIU Pharmacology Graduate Program Committee 1986-1989 SIU Radiological Control Committee 1986-1988 SIU Institutional Biosafety Committee

Stephen P. Arneric, Ph.D. – April, 2015 8

Editorial Boards

CNS Drugs Review Ad Hoc Reviewer: Biochemical Pharmacology Brain Research Current Patents Developmental Brain Research Drug Development Research Experimental Neurology Journal of Cerebral Blood Flow and Metabolism Journal of Medicinal Chemistry Journal of Pharmacology and Experimental Therapeutics Life Sciences Neurobiology of Aging Neurochemistry Neuroscience Neuroscience Letters Pain Pharmacology Biochemistry Behavior Psychopharmacology Ad Hoc Grant Reviewer: American Heart Association Department of Veterans Affairs National Science Foundation Wellcome Trust, U.K.

Stephen P. Arneric, Ph.D. – April, 2015 9

PATENTS

1. Garvey, D.S., Carrera, G.M., Arneric, S.P., Shue, Y-K., Lin, N-H., He, Y. Isoxazole and isothiazole compounds that enhance cognitive function. Application filed May 1991 [Docket # 4996- WO 9221339]

2. Garvey, D.S., Carrera, G.M., Lee, E.L., Lebold, S.A., Arneric, S.P., Shue, Y-K., Lin, N-H., He,

Y. Isoxazole, isothiazole and pyrrazole compounds that enhance cognitive function. US 5,409,946; Issued April 25, 1995

3. Arneric, S.P., Decker, M.W. (+)-2-Methylpiperidine as Modulator of Cholinergic Systems, US 5,272,155; Issued December 21, 1993

4. Franke, H., Hoffman, G, Kindel H, Arneric, S.P., Sullivan, J.P., and Cannon, Transdermal

therapeutic system for dispensing (S)-3-methyl-5-(1-methyl-2-pyrrolidenyl)-isoxazole or one of its pharmaceutically acceptable salts. WO 9621434 A1; Published: July 18, 1996.

5. Arneric, S.P., Dart, M., Holladay, M.W, Lynch, J., Ryther, K., Sullivan, J.P., et al., 3-pyridyl

enantiomers and their use as analgesics. 6013.US.01, Filed: December 10, 1996. 6. Arneric, S.P. and Andersson, P-O., Pharmaceutical Composition. PCT/SE02/01748.

Application number 09/965,556. Filed: September 27, 2002 7. Nixon, P.R., Systma, J.A., Franz, R.M., Lucisano, L., Eller, M.G., Meurgey, F.M., Arneric, S.P.,

Sustained-Release Alprazolam Composition. 10/179,706, Filed: June 25, 2002.

8. Arneric, S.P. The use of 4-Phenyl-substituted tetrahydroisoquinolines in the treatment of pain, migraine headaches, and urinary incontinence. US60/430,242, Filed: December 2, 2002.

9. Arneric, S.P. The use of 4-Phenyl-substituted tetrahydroisoquinolines in the treatment of pain, migraine headaches, and urinary incontinence. US60/430,298, Filed: December 2, 2002.

10. Arneric, S.P. The use of Aryl- and Heteroaryl-substituted tetrahydroisoquinolines in the treatment of chronic and neuropathic pain, migraine headaches, and urge, stress and mixed urinary incontinence. US 60/430,285, Filed: December 2, 2002.

11. Arneric, S. P. et al. Method for treatment of depression and anxiety disordrs by combination therapy. US 60/502,304, Filed September 12, 2003.

12. Arneric, S. P. et al. Compositions of a cyclooxegenase-2 selective inhibitor and an anticonvulsant agent for the treatment of central nervous system disorders. US 10/862,846, Filed June 7, 2004.

13. Arneric, S. P. et al. Benzenesulfonaminde or methylsulfonylbenzene cyclooxegenase-2

selective inhibitor and a colinergic agent for thetreatment of reduced blood flow or trauma to the central nervous system. US 10/845,574, Filed May 13, 2004.

14. Arneric, S. P. et al. Compositions of a chromene cyclooxegenase-2 selective inhibitor and a colinergic agent for thetreatment of reduced blood flow or trauma to the central nervous system. US 10/845,012, Filed May 13, 2004.

15. Arneric, S. P. et al. Compositions of a cyclooxegenase-2 selective inhibitor and a colinergic agent for thetreatment of reduced blood flow or trauma to the central nervous system. US 10/844,921, Filed May 13, 2004.

Stephen P. Arneric, Ph.D. – April, 2015 10

INVITED PRESENTATIONS (since 1993) "Nicotinic cognition enhancing agents improve performance by facilitating basal forebrain neurons governing cortical CBF", BRAIN '93, Sendai, Japan, May 1993. "Nicotinic agonists in Alzheimer's Disease: Does the molecular diversity of nicotine receptors offer the opportunity for developing CNS selective cholinergic channel activators?" Recent Advances In The Treatment of Neurodegenerative Disorders and Cognitive Dysfunction, Capri, Italy, May 1-3, 1993. "Cholinergic channel activators (ChCAs) as therapeutics for CNS disorders: ABT 418 [(S)-3-methyl-5-(1-methyl-2-pyrrolidinyl) isoxazole hydrochloride] as a prototype ChCA to treat Alzheimer's disease (AD)." XIXth CINP Congress, Washington, D.C., 1994. "Development of novel cholinergic channel activator (ChCA) compounds: A new therapeutic approach for the treatment of CNS disorders", Cholinergic Signalling in Alzheimer's Disease: Therapeutic Strategies, Sept. 4-8, 1994, Vienna, Austria. "Cholinergic channel activators (ChCAs) for the treatment of Alzheimer's disease." IBC Conference: Alzheimer's Disease-Advances in Understanding and Treatment, Philadelphia, PA., September 22-23, 1994. "Molecular diversity of nicotinic acetylcholine receptors: Opportunities for the development of ligands for the treatment of CNS disorders." Soc. for Research on Nicotine and Tobacco, San Diego, CA, March 23, 1995. "Molecular diversity of nAChRs: Opportunities for the development of cholinergic channel modulators for treatment of CNS disorders." International Symposium on Neuronal Receptor Mechanisms, Niigata, Japan, June 28-29., 1995. "Cytoprotective and cognitive enhancement actions of ABT-418 in primates" XVIIth Int. Symposium on Cerebral Blood Flow and Metabolism, Cologne, Germany, July 2-6, 1995. "Neuronal nicotinic acetylcholine receptor (nAChR) diversity and therapeutic potential of selective ligands." Chairman/Organizer of Med. Chem. Symposium, American Chemical Soc., Chicago IL, August 1995. "ABT-089: An orally active cholinergic channel modulator (ChCM) with cognition enhancing and neuroprotective properties." American College Neuropsychopharmacology, San Juan, Puerto Rico, Dec. 1995. "ABT-089: An orally active cholinergic channel modulator (ChCM) with cognition enhancing and neuroprotective activity." Fourth International Nice/Springfield Symposium on Advances in Alzheimer's Therapy. Nice France, April 10-14, 1996. "Cholinergic channel modulators(ChCMs) for the treatment of cognitive and neurodegenerative disorders." IBC Conference: Alzheimer's Disease-Advances in Understanding and Treatment, Oak Brook, IL., June 17-18, 1996. "Therapeutic opportunities for cholinergic channel modulators(ChCMs) to treat CNS disorders." Duke University Nicotine Symposium, Raleigh, N.C., Nov. 15, 1996. "Cholinergic channel modulators (ChCMs) for the treatment of cognitive and neurodegenerative disorders" Alzheimer's Disease: Advancing Therapeutics Towards the Clinic, Washington, DC., June 16-17, 1997.

Stephen P. Arneric, Ph.D. – April, 2015 11

"The therapeutic potential of modulators of functional and dysfunctional neuronal nicotinic acetylcholine receptors (nAChRs)" IBC Conference: Nicotinic Acetylcholine Receptor Therapeutics, Washington, DC., July 24-25, 1997. “Cholinergic channel modulators (ChCMs) for the potential treatment of acute and neuropathic pain” New Therapeutic Strategies in the Treatment of Pain, Washington, D.C., October 6-7, 1997. “Modulation of functional and dysfunctional neuronal nAChRs” Molecular Basis of Nicotine Pharmacology, New Orleans, October 25, 1997. "ABT-594: A broad sprectrum, non-opioid analgesic acting by neuronal nicotinic acetylcholine receptors" Therapeutic Developments for Chronic Pain, Annapolis, Maryland, May 18-20, 1998. “Therapeutic opportunities for neuronal nicotinic acetylcholine receptor modulators” Neuronal Nicotinic Receptors: From Structure to Therapeutics, Venice, Italy, Oct. 1-4, 1999. “Nicotine Receptors: Modulation by Nicotine” ACNP, December, 2006. “nAChR Drug Discovery: Then, Now and the Future” Soc. For Neuroscience, November, 2007. "T-type calcium (Cav3) channels as pharmacological targets for treating pain" , Spring Pain Meeting, Grand Cayman, 2008. “nAChRs in Drug Discovery: Evolving Opporunities and Challenges”, Nicotinic Acetylcholine Receptor-Based Therapeutics: Emerging Frontiers in Basic Research & Clinical Science, Satellite of Society for Neuroscience, Oct. 14, 2009. “From the lab to the clinic: why do so many promising pain relievers fail?” Pain Day, Oregon Health Sciences University, February 29, 2012. “Delivering Chronic Pain Therapeutics: What’s Been Lost in Translation? GTC’s Pain Research & Therapeutics, San Francisco, September 13, 2012. “Tailoring Treatments to Sustain the Aged Wellderly: Facts, Challenges & Future” Healthy Aging Conference, Portland, Oregon, October 10, 2012. “Failed Analgesic Studies: 10 Factors Diminishing Translational Success” Pain Therapeutics Summit –East (Boston, MA, Sept. 25-26, 2013) & Pain Therapeutics Summit- West (San Diego, CA, Nov. 8-9, 2013. “Strategies for new target development of pain therapeutics” SIMPAR-2014, Rome, Italy, March 28, 2014 Discussion Panelist for a webinar by William Schmidt “Building a Better Aspirin: The Frontiers of Pain Medicine Development”, Sept 10, 2014.

Stephen P. Arneric, Ph.D. – April, 2015 12

PEER REVIEWED PUBLICATIONS 1. McCormack, K.M., Arneric, S.P. and Hook, J.B. Action of exogenously administered steroid

hormones following perinatal exposure to polybrominated bipheyls J. Toxicol. Environ. Health 5:1085-1094, 1979.

2. Arneric, S.P., McCormack, K.M., Braselton, W.E., Jr. and Hook, J.B. Altered metabolism of

progesterone by hepatic microsomes from rats following dietary exposure to polybrominated biphenyls. Toxicol. Appl. Pharmacol. 4:187-196, 1980.

3. Arneric, S.P., Goodale, D.B., Flynn, J.R. and Long, J.P. Rapid and simple analysis of DOPA and

5-HTP using high performance liquid chromatography with electrochemical detection. Brain Res. Bull. 6:407-411, 1981.

4. Maixner, W., Arneric, S.P., Abou Zeit-Har, M.S., Lecompte, J., Verimer, T. Cannon, J.G., Lee, T.

and Long, J.P. Pharmacological effects of 2-amino-tetralins, octahydrobenzo(f)quinolines, and clonidine on the isolated guinea pig ileum. Eur. J. Pharmacol. 71:483-488, 1981.

5. Verimer, T., Arneric, S.P., Long, J.P., Walsh, B.J. and Abou Zeit-Har, M.S. Effects of

ovariectomy, castration and chronic lithium chloride treatment on stereotyped behavior in rats. Psychopharmacol.75:273-276, 1981.

6. Verimer, T., Long, J.P., Koble, D.L., Cannon, J.G., Flynn, J.R., Goodale, D.B. and Arneric, S.P.

Dopamine receptor stimulating activity of hydroxy-6-methyl-2-aminotetralin derivatives. Arch. Int. Pharmacodyn 250:221-241, 1981.

7. Verimer, T., Long, J.P., Flynn, J.R., Arneric, S.P. and Walsh, B.J. Sub-sensitivity of the

presynaptic dopamine receptors in cat heart after the termination of chronic haloperidol treatment. Arch. Int. Pharmacodyn. 253:233-240, 1981.

8. Sindelar, R.D., Mott, J., Barfknecht, C.F., Arneric, S.P., Flynn, J.R. and Long, J.P. 2-amino-4,7-

dimethoxyindane derivatives: Synthesis and assessment of dopaminergic and cardiovascular actions. J. Med. Chem. 25:858-864, 1982.

9. Arneric, S.P., Roetker, A. and Long, J.P. Potent anorexic-like effects of RDS-127 (2-di-n-

propylamino- 4,7-dimethoxyindane) in the rat: a comparison with other dopamine agonists. Neuropharmacology 21:685-690, 1982.

10. Arneric, S.P., Maixner, W., Long, J.P., Mott, J., Barfknecht, C.F., Perez, J.A. and Cannon, J.G.

Structure activity relationships of 2-amino-tetralin and 2-aminoindanes: Inhibitory neuro-effector mechanisms in isolated guinea pig ilea. Arch. Int. Pharmacodyn. 258:84-99, 1982.

11. Arneric, S.P., Roetker, A., Long, J.P., Mott, J. and Barfknecht, C.F. Effects of semirigid

Methoxamine analogs on vascular smooth muscle: studies of methoxy-2-aminotetralin and 2-aminoindane derivatives. Arch Int. Pharmacodyn. 257:263-273, 1982.

12. Arneric, S.P., Collins, E., Bhatnagar, R.K. and Long, J.P. Is domperiodone a selective peripheral

dopamine receptor antagonist? Neuropharmacology 21:1317-1321, 1982. 13. Clark, J.T., Smith, E.R., Stefanich, M.L., Arneric, S.P., Long, J.P. and Davidson, J.M. Effects of

a novel dopamine-receptor agonist, RDS-127 (2-di-n-propylamino- 4,7-dimethoxyindane), on hormones and sexual behavior in the male rat. Physiol. Behav. 29:1-6, 1982.

Stephen P. Arneric, Ph.D. – April, 2015 13

14. Bhatnagar, R.K., Arneric, S.P., Cannon, J.G., Flynn, J.R. and Long, J.P. Structure activity relationships of presynaptic dopamine receptor agonists. Pharmacol. Physiol. & Behav. 17(1):11-19, 1982.

15. Arneric, S.P., Long, J.P., Williams, M., Goodale, D.B., Mott, J., Lakoski, J.M., Gebhart, G.F.

RDS-127 (2-di-n-propylamino- 4,7-dimethoxy-indane): Central effects of a new dopamine receptor agonist. J. Pharmacol. Exp. Ther. 224:161-170, 1983.

16. Arneric, S.P. and Long, J.P. RDS-127: An alternative approach to developing dopamine

receptor agonists with central presynaptic actions following oral administration: A comparison with apomorphine, bromocriptine and the novel compound RDS-127. Drug Develop. Res. 3(3):221-232, 1983.

17. Maixner, W., Flynn, J.R., Arneric, S.P., Koons, J.C., Cannon, J.G. and Long, J.P. II.

Pharmacological studies with derivatives of 2-aminotetralin, benzo(f)quinoline, apomorphine and clonidine suggest a pharmacological dissimilarity between peripheral presynaptic dopamine and alpha receptors. J. Pharmacol. Exp. Ther. 224(2):352-358, 1983.

18. Arneric, S.P., Chow, S.A., Long, J.P. and Fischer, L. Dopamine analog-induced hyperglycemia

in rats involves the adrenal medulla and the endocrine pancreas: correlations of hyperglycemia with other dopaminergic actions. J. Pharmacol. Exp. Therap. 228(3):551-559, 1984.

19. Arneric, S.P., Chow, S., Bhatnagar, R.K., Webb, R., Fischer, L.J. and Long, J.P. Evidence that

central mechanisms modulate sympathetic neuronal activity to the adrenal medulla to alter glucoregulatory mechanisms in the rat. Neuropharmacology 23:137-147, 1984.

20. Arneric, S.P., Chow, S.A., Long, J.P., and Fischer, L.J. Inhibition of insulin release from rat

pancreatic islets by dopamine analogs: evidence for two types of inhibitors. Diabetes 33(9):888-893, 1984.

21. Arneric, S.P. and Long, J.P. RDS-127 (2-di-n-propylamino- 4,7-dimethoxy-indane): Evidence

that some cardiovascular effects of a novel dopamine receptor agonist are mediated centrally. J. Pharm. Pharmacol. 36:318-321, 1984.

22. Arneric, S.P. and Reis, D.J. Somatostatin and cholecystokinin octapeptide differentially

modulate release of 3H-acetylcholine from caudate nucleus but not cerebral cortex: role of dopamine receptor activation. Brain Res. 374:153-161, 1986.

23. Iwata, J., LeDoux, J.E., Meeley, M.P. Arneric, S.P. and Reis, D.J. Intrinsic neurons in the

amygdaloid field projected to by the medial geniculate body mediate emotional responses classically conditioned to acoustic stimuli. Brain Res. 383:195-214, 1986.

24. Arneric, S.P., Iadecola, C., Honig, M.A., Underwood, M.D. and Reis, D.J. Local cholinergic

mechanisms mediate the cortical vasodilation elicited by electrical stimulation of the fastigial nucleus. Acta Physiologica Scand. 127(Suppl. 552):70-73, 1986.

25. Arneric, S.P., Meeley, M.P. and Reis, D.J. Somatostatin and CCK-8 modulate release of striatal

amino acids: role of dopamine receptors. Peptides 7:97-103, 1986. 26. Arneric, S.P., Meeley, M.P. and Reis, D.J. m-Enkephalin selectively increases the spontaneous

release of amino acid neurotransmitters from rat striatal slices. Neurosci. Lett. 66:73-78, 1986.

27. Arneric, S.P., Meeley, M.P. and Reis, D.J. Ca2+-dependent release of tyrosine in brain elicited by neuropeptide receptors. J. Neurochem. 48:1581-1589, 1987.

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28. Arneric, S.P., Iadecola, C., Underwood, M.D. and Reis, D.J. Local cholinergic mechanisms participate in the increase in cortical cerebral blood flow elicited by electrical stimulation of the fastigial nucleus in rat. Brain Res. 411:212-225, 1987.

29. Iadecola, C., Arneric, S.P., Baker, H.D., Tucker, L.W. and Reis, D.J. Role of local neurons in

the cerebrocortical vasodilation elicited from cerebellum. Am. J. Physiol. 252:R1082-R1091, 1987.

30. Arneric, S.P., Woo, J.I., Meeley, M.P. and Reis, D.J. Spontaneous release of endogenous

aspartate and glutamate from rat striatal slices is increased following destruction of local neurons by ibotenic acid. Neurochem. Res. 13(5):423-428, 1988.

31. Arneric, S.P., Honig, M.A., Milner, T.A., Greco, S., Iadecola, C. and Reis, D.J. Neuronal and

endothelial sites of acetylcholine synthesis and release associated with microvessels in rat cerebral cortex: ultrastructural and neurochemical studies. Brain Res. 454:11-30, 1988.

32. Ernsberger, P., Arneric, S.P., Arango, V. and Reis, D.J. Quantitative distribution of muscarinic

receptors and choline acetyltransferase in rat medulla: examination of transmitter-receptor mismatch. Brain Res. 452:336-344, 1988.

33. Iadecola, C., Arneric, S.P. and Reis, D.J. Local and remote microvascular changes in

excitotoxin-induced focal brain lesions. Brain Res. 501:188-193, 1989. 34. Arneric, S.P. Cortical cerebral blood flow is modulated by cholinergic basal forebrain neurons:

effects of ibotenic acid lesions and electrical stimulation. In: Neurotransmission and Cerebrovascular Function, Vol. 1, Excerpta Medica International Congress Series (eds. J. Seylaz and E.T. Mackenzie), pp. 381-384, 1989.

35. Arneric, S.P., Guiliano, R., Ernsberger, P., Underwood, M.D. and Reis, D.J. Synthesis, release

and receptor binding of acetylcholine in the area of the rostral ventrolateral medulla: contributions in regulating arterial pressure. Brain Res. 511:98-112, 1990.

36. Iadecola, C., Arneric, S.P., Baker, H.D., Callaway, J. and Reis, D.J. Maintenance of local

cerebral blood flow after acute neuronal death: possible role of non-neuronal cells. Neuroscience, 1990.

37. Caspary, D.M., Raza, A., Lawhorn-Armour, B.A., Pippin, J., and Arneric, S.P.

Immunocytochemical and neurochemical evidence for age-related loss of GABA in the inferior colliculus: implications for neural presbycusis. J. Neurosci. 10:2363-2372, 1990.

38. Tingley, F.D. and Arneric, S.P. Evidence for clonidine presynaptically modulating amino acid

release in the rostral ventral medulla: role in hypertension. Brain Res. 573:175-181, 1990. 39. Linville, D. and Arneric, S.P. Cortical cerebral blood flow governed by basal forebrain neurons:

age-related impairments in rats. Neurobiol. Aging 12(5): 503-510, 1991. 40. Somani, S.M., Babu, S.R., Arneric, S.P., and S.N. Dube. Effect of cholinesterase inhibitor and

exercise on choline acetyltransferase and acetylcholinesterase activities in rat brain regions. Pharmacol. Biochem. & Behav. 39(2): , 1991.

41. Anderson, D.J., Decker, M.W., Cadman, E., Buckley, M.J., Vella-Rountree, L., Arneric, S.P., and

Williams, M. The aminopyridazine muscarinic agonist, SR 95639A, is a functional M2 receptor antagonist in rat brain. Drug Dev. Res. 24(1):107-118, 1991.

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42. Faingold, C.L., Naritoku, D.K., Copley, C.A., Randall, M.E., Riaz, A., Anderson, C.A.B. and Arneric, S.P. Glutamate in the inferior colliculus plays a critical role in audiogenic seizure initiation. Epilepsy Res. 13: 95-105, 1992.

43. Linville, D.G., Giacobini, E., and Arneric, S.P. Heptyl-physostigmine enhances basal forebrain

control of cortical cerebral circulation, J. Neurosci. Res. 31: 573-577, 1992. 44. Raszkiewicz, J., Linville, D. G. , Kerwin, J.K., Jr., and Arneric, S.P. Nitric oxide synthase is

critical in mediating increases in cortical cerebral circulation elicited by basal forebrain stimulation. J. Neurosci. Res. 33: 129-135, 1992.

45. Giordano, T., Pan, J.B., Casuto, D., Arneric, S.P. and Watanabe, S., Thyroid hormone regulation

of NGF, NT-3 and BDNF RNA in the adult rat brain, Mol. Brain Res., 16: 239-245, 1992. 46. Brioni, J.D., Curzon, P. , Buckley, M.J., Arneric, S.P., and Decker, M.W., Linopirdine (DuP996)

facilitates the retention of avoidance training and improves performance of septal-lesioned rats in the water maze. Pharmacol. Biochem. Behavior. 44: 37-43, 1993.

47. Brioni, J.D. and Arneric, S.P. Nicotinic receptor agonists facilitate retention of avoidance training:

participation of dopaminergic mechanism. Behavioral and Neural Biology. 59: 57-62, 1993. 48. Decker, M.W., Majchrzak, M.J. and Arneric, S.P. Effects of lobeline, a nicotinic receptor agonist,

on learning and memory, Pharmacol. Biochem. Behavior. 45:571-576, 1993. 49. Linville, D.G., Williams, S., Raszkiewicz, J.L. and Arneric, S.P. Nicotinic agonist modulate basal

forebrain control of cortical cerebral blood flow, J. Pharmacol. Exp. Therapeutics 267: 440-448, 1993.

50. Linville, D.G., Williams, S. and Arneric, S.P., Basal forebrain control of cortical cerebral blood

flow is independent of local cortical neurons, Brain Res. 662: 26-34, 1993. 51. Monteggia,L. M., Arneric, S.P. and Giordano, T. Nicotine effects on the regulation of amyloid

precursor protein splicing, neurotrophin and glucose transporter RNA levels in aged rats Int. J. Develop. Neurosci. 12: 133-142, 1994.

52. Anderson, D.J. and Arneric, S.P. Nicotinic receptor binding of [3H]cytisine, [3H]nicotine, and

[3H]methylcarbamylcholine in rat brain Eur. J. Pharmacol.,253: 261-267, 1994. 53. Decker, M.W., Majchrzak, M.J., Cadman, E.D. and Arneric, S.P. Effects of chlorisondamine on

nicotinic receptor binding in whole brain and nicotine-induced changes in locomotor activity in rats. Drug Dev. Res. 31: 89-94, 1994.

54. Faingold, C.L., Marcinczyk, M.J., Casebeer, D.J., Randall, M.E. Arneric, S.P., and Browning,

R.A., GABA in the inferior colliculus plays a critical role in control of audiogenic seizures. Brain Res. 640:40-47, 1994.

55. Raza, A., Milbrandt, J.C., Arneric, S.P. and Caspary, D.M., Age-related changes in brainstem

auditory neurotransmitters: measures of GABA and acetylcholine function Hearing Res 77: 221-230, 1994.

56. Arneric, S.P., Sullivan, J.P., Briggs, C.A., Donnelly - Roberts, D., Anderson, D.J., Raszkiewicz,

J.L., Hughes, M., Cadman, E.D., Adams, P., Garvey, D.S., Wasicak, J. and Williams, M., ABT- 418 : A novel cholinergic ligand with cognition enhancing and anxiolytic activities: I. In vitro characterization , J. Pharmacol. Exp. Therap. 270: 310-318, 1994.

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57. Decker, M.W., Brioni, J.D., Sullivan, J.P., Buckley, M.J., Raded, R.J., Raskiewicz, J.L., Kang,

C.H., Kim, D.J.B., Giardina, W.J., Wasicak, J., Garvey, D.S., Williams, M., and Arneric, S.P. ABT- 418: A novel cholinergic channel ligand with cognition and anxiolytic activities: II. In vivo characterization. J. Pharmacol. Exp. Therap., 270: 319-328, 1994.

58. Garvey, D.S., Wasicak, J., Decker, M.W., Brioni, J.D., Buckley, M.J., Sullivan, J.P., Carrera, G.,

Holladay, M.H., Arneric, S.P., and Williams, M., Novel isoxazoles which interact with brain cholinergic channel receptors have instrinsic cognitive enhancing and axiolytic activities. J. Med. Chem. 37:1055-1059, 1994.

59. Decker, M.W., Curzon, P., Brioni J.D., and Arneric S.P. Effects of ABT- 418, a novel

cholinergic channel ligand, on place learning in septal- lesioned rats Eur J Pharmacol 261: 217-222, 1994.

60. Brioni, J.D., O'Neill, A.B., Kim, D.J.B., Decker, M.W., Sullivan, J.P. and Arneric, S.P. Anxiolytic-

like effects of the novel cholinergic channel activator, ABT-418. J Pharmacol Exp Therapeutics 271:353-361, 1994.

61. Rodrigues, A.D., Ferrero, J.L., Amann, M.T., Rotert, G.A., Cepa, S.P., Surber, B.W., Machinist,

J.M., Sullivan, J.P., Garvey, D.S., Fitzgerald, M. and Arneric, S.P., The in vitro hepatic metabolism of ABT-418, a cholinergic channel activator, in rat, dog, cynomolgus monkey and human. Drug Metabolism & Disposition 22: 788-798, 1994.

62. Sullivan, J.P., Briggs, C.A., Donnelly-Roberts, D., Brioni, J.D., Radek, R.J., McKenna, D.G.,

Campbell, J.E., Arneric, S.P., Decker, M.W., and Bannon, A.W., (±)-Epibatidine can differentially evoke responses elicited by putative subtypes of nicotinic acetylcholine receptors (nAChRs), Med. Chem. Res. 4:502-516, 1994.

63. Garvey, D.S., Wasicak, J.T., Elliott, R.L., Lebold, S., Hettinger, A.-M., Carrera, G.M., Lin, N.-H.,

He, Y., Holladay, M.W., Anderson, D.J., Cadman, E.D., Raszkiewicz, J.L., Sullivan, J.P., and Arneric, S.P., Ligands for brain cholinergic channel receptors: synthesis and in vitro characterization of novel isoxazoles and isothiazoles as bioisosteric replacements for the pyridine ring in nicotine, J. Med. Chem. 37:4455-4463, 1994.

64. Brioni, J.D.,Kim, D.J.B., Brodie, M.S., Decker, M.W., and Arneric, S.P. , ABT-418: Discriminative

stimulus properties and effect on ventral tegmental cell activity, Psychopharmacol. 107: 368-375, 1995.

65. Briggs, C.A., Hughes, M.L., Monteggia, L.M., Giordano, T., Donnelly-Roberts, D. and Arneric,

S.P., Ganglionic nicotinic acetylcholine receptor activation by the novel agonist ABT- 418, Drug Development Res., 34: 39-46, 1995.

66. Sullivan, J.P., Decker, M.W., Brioni, J.D., Roberts-Donnelly, D., Anderson, D.J., Bannon, A.,

Gopalakrishnan, M., Piattoni-Kaplan, M., Adams, P., Buckley, M.J., Kang, C.H., Williams, M., and Arneric, S.P., Pharmacological properties of (±)-Epibatidine: A potent nicotinic acetylcholine receptor ligand., J. Pharmacol. Exp. Therap. 271: 624-631, 1995.

67. Anderson, D.J., Williams, M., Arneric, S.P., Pauly, J.R., Rotert, G.A., Suber, B., Raszkiewicz,

J.L., Wasicak, J., and Sullivan, J.P., Characterization of [3H]ABT-418: A novel cholinergic channel ligand. J. Pharmacol. Exp. Therap. 273: 1434-1441, 1995.

68. Monteggia, L.M., Gopalakrishnan, M., Touma, E., Idler, K.B., Nash, N., Arneric, S.P., Sullivan,

J.P. and Giordano, T., Cloning and transient expression of genes encoding the human and neuronal nicotinic acetylcholine receptor (nAChR) subunits. Gene 155: 189-193, 1995.

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69. Bannon, A.W., Gunther, K.L., Decker, M.W. and Arneric, S.P., The influence of BAY K8644

treatment on (±)-epibatidine-induced analgesia Brain Res. 678: 244-250, 1995. 70. Decker, M.W., Anderson, D.J., Brioni, J.D., Donnelly-Roberts, D., Kang, C.-H., O'Neill, A.,

Swanson, S., Arneric, S.P., and Sullivan, J.P., In vitro and in vivo characterization of erysodine, an erythrina alkaloid with competitive antagonist properties at neuronal nicotinic acetylcholine receptors, Eur. J. Pharmacol. 280: 79-89, 1995.

71. Buccafusco, J.J., Jackson, W.J., Terry Jr., A.V., Marsh, K.C., Decker, M.W., and Arneric, S.P.

Improvement in performance of a delayed matching-to-sample task by monkeys following ABT-418: A novel cholinergic channel activator for memory enhancement. Psychopharmacol. 120: 256-266, 1995.

72. Gopalakrishnan, M., Bertrand, D., Touma, E. Giordano, T., Campbell, J., Hu, I.C., Buisson, B.,

Donnelly-Roberts, D., Arneric, S.P., and Sullivan, J.P., Pharmacological characterization of the

human 7 neuronal nicotinic acetylcholine receptor subtype stably expressed in a mammalian cell line. Eur. J. Pharmacol., 290: 237-246, 1995.

73. Wevers, A., Sullivan, J.S., Giordano, T., Ch. Birtsch, N.N., Nowacki, S., Arneric, S.P., and H.

Schroder, Cellular distribution of the mRNA for the subunit of the nicotinic acetylcholine receptor in the human cerebral cortex. Drug Dev. Res. 36: 103-110, 1995.

74. Lin, N.H., He,Y., Arneric, S.P. and Sullivan, J.P., Synthesis and structure-activity relationships of

2'-(R) and (S) pyrrolidine-modified analogs of the cholinergic channel activator, ABT-418. Bioorganic & Medicinal Chem. Lett. 5: 1141-1146, 1995.

75. Turek, J.W., Kang, C.H., Campbell, J.E., Arneric, S.P. and Sullivan, J.P., A sensitive technique

for the detection of the neuronal nicotinic acetylcholine receptor antagonist, methyllycaconitine, in rat plasma and brain. Neurosci. Methods 61: 113-118, 1995.

76. Donnelly-Roberts, D., Arneric, S.P. and Sullivan, J.P., Functional modulation of human

"ganglionic-like" neuronal nicotinic acetylcholine receptors (nAChRs) by L-Type Calcium Channel Antagonists. Biochem. Biophysc. Res. Comm. 213: 657-662, 1995.

77. Gopalakrishnan, M., Monteggia, L.M., Anderson, D.J., Arneric, S.P., and Sullivan, J.P., Stable

expression, pharmacologic properties and regulation of the human nicotinic acetylcholine

receptor. J. Pharmacol. Exp. Therap. 276: 289-297,1996. 78. Donnelly-Roberts, D.L., Xue, I., Arneric, S.P. and Sullivan, J.P. In vitro neuroprotective

properties of the novel cholinergic channel activator (ChCA), ABT-418. Brain Res. 719: 36-44, 1996.

79. Radek, R.J., Briggs, C.A., Sullivan, J.P., Kang, C.H. and Arneric, S.P. Effects of the cholinergic

channel activator ABT-418 on cortical EEG: comparison with (-)-nicotine. Drug Dev. Res. 37: 73-79, 1996.

80. Sullivan, J.P., Donnelly-Roberts, D., Briggs, C.A., Anderson, D.J., Gopalakrishnan, M., Piattoni-

Kaplan, M., Campbell, J.E., McKenna, D.G., Molinari, E., Hettinger, A.M., Garvey, D.S., Wasicak, J., Holladay, M.W., Williams, M. and Arneric S.P. A-85380 [3-(2(S)-Azetidinylmethoxy)Pyridine]:

In vitro pharmacological properties of a novel, high affinity nicotinic acetylcholine receptor ligand. Neuropharmacol. 35(6): 725-734, 1996.

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81. Abreo, M.A., Lin, Nan-Horng, Garvey, D.S., Gunn, D.E., Hettinger, A.M., Wasicak, J.T., Pavlik,

P.A., Martin, Y.C., Donnelly-Roberts, D., Anderson, D.J., Sullivan, J.P., Williams, M., Arneric, S.P., Holladay, M.W. Novel 3-pyridyl ethers with subnanomolar affinity for central neuronal nicotinic acetylcholine receptors. J. Med. Chem. 39:817-825, 1996.

82. Buisson, B., Gopalakrishnan, M., Arneric, S.P., Sullivan, J.P., Bertrand, D. Human neuronal nicotinic acetylcholine receptors in HEK 293 cells: a patch clamp study. J. Neurosci. 16 (24): 7880-7891, 1996.

83. Elliott, R.L., Kopecka, H., Gunn, D.E., Lin, N.H., Garvery, D.S., Ryther, K.E., Holladay, M.W.,

Anderson, D.A., Campbell, J.E., Sullivan, J.P., Buckley, M., Gunther, K.L., O'Neill, A.B., Decker, M.W., and Arneric, S.P., 2-(Aryloxymethyl) azacyclic analogues as novel nicotinic acetylcholine receptor (nAChR) ligands, Biochem. Med. Chem. Commun. 6(19): 2283-2288, 1996.

84. Briggs, C.A., Anderson, D.J., Brioni, J.D., Buccafusco, J.J., Buckley, M.J., Campbell, J.E.,

Decker, M.W., Donnelly-Roberts, D., Elliott, R.L., Holladay, M.W., Hui, Y.H., Jackson, J.J., Kim, D.J.B., Marsh, K.C., O'Neill, A., Prendergast, M.A., Ryther, K.B., Sullivan, J.P. and Arneric, S.P., Functional characterization of the novel neuronal nicotinic acetylcholine receptor ligand GTS-21 in vitro and in vivo. Pharmacol. Biochemistry and Behavior 57: 231-241, 1997.

85. Prendegast, M.A., Terry, Jr., A.V., Jackson, W.J., Marsh, K.C., Decker, M.W., Arneric, S.P., and

Buccafusco, J.J. Improvement in accuracy on a delayed recall in aged and non-aged monkeys after intramuscular or transdermal administration of CNS nicotinic receptor agonist, ABT-418. Pyschopharmacology 130: 276-284, 1997.

86. Lin, N-H., Gunn, D.E., Ryther, K.B., Garvey, D.S., Donnelly-Roberts, D.L., Decker, M.W., Brioni,

J.D., Buckley, M.J., Rodrigues, A.D., Marsh, K.G., Anderson, D.J., Sullivan, J.P., Williams, M., Arneric, S.P. and Holladay, M.W. Structure-activity studies on ABT-089: an orally bioavailable 3-pyridyl ether cholinergic channel modulator with cognition enhancing properties. J. Med. Chem. 40: 385-390, 1997.

87. Brioni, J.D., Kim, D.J.B., O’Neill, A., Brodie, M.S., Decker, M.W., and Arneric, S.P. ABT-089 [2-

Methyl-3-(2-(S)-pyrrolidinylmehthoxy) pyridine dihydrochloride]: Discriminative stimulus properties and electrophysiological actions. Drug Dev. Res. 40: 259-266, 1997.

88. Reganthan, M., Gopalakrishnan, M., Messi, M.L., Arneric, S.P., Sullivan, J.P., and DelBono, O.,

Regulation of intracellular calcium by ABT-418: Involvement of the human neuronal nicotinic acetylcholine receptor. Brain Res. (In Press) 1997.

89. Decker, M.W., Bannon, A.W., Curzon, P., Gunther, K.L., Brioni, J.D., Holladay, M.W., Lin, N-H.,

Li, Y., Daanen, J.F., Buccafuscio, J.J., Prendergast, M.A., Jackson, W.J., and Arneric, S.P., ABT-089 [2-Methyl-3-(2-(S)-pyrrolidinylmethoxy)pyridine dihydrochloride]: II. A novel cholinergic channel modulator with effects on cognitive performance in rats and monkeys. J. Pharmacol. Exp. Therap. 283: 247-258, 1997.

90. Sullivan, J.P., Donnelly-Roberts, D., Briggs, C.A., Anderson, D.J., Gopalakrishnan, M., Xue, I.C.,

Piattoni-Kaplan, M., Molinari, E., Campbell, J.E., McKenna, D.G., Gunn, D.E., Lin, N-H., Ryther, K.B., He, Y., Holladay, M.W., Wonnacott, S., Williams, M., and Arneric, S.P., ABT-089 [2-Methyl-3-(2-(S)-pyrrolidinylmethoxy)pyridine dihydrochloride]: II. A potent and selective cholinergic channel modulator with neuroprotective properties. J. Pharmacol. Exp. Therap. 283: 235-246, 1997.

Stephen P. Arneric, Ph.D. – April, 2015 19

91. Arneric,. S.P., Campbell, J.E., Sullivan, J.P., Arnold, W., He, Y., Holladay, M.W., Lin, N.H.,

Daanen, J., Li, Y., Marsh, K.C., Peterson, B., Nellans, H., Trevidi, J., Sullivan, J.P., and Williams, M. ABT-089 [3-(2(S)-Pyrolidinylmethoxy)-2-methyl-pyridine]: An orally effective cholinergic channel modulator with potential once-a-day dosing and cardiovascular safety Drug Dev. Res. 41:31-43, 1997.

92. Puttfarcken, P.S., Manelli, A.M., Arneric, S.P., and Donnelly-Roberts, D., Evidence for nicotinic

receptors potentially modulating nociceptive transmission at the level of the dorsal root ganglion: Studies with F11 cells. J. Neurochem. 69: 930-938, 1997.

93. Qiu, Y., Flood, K, Marsh, K., Carroll, S., Trivedi, J., Arneric, S.P., and Krill, S.L., Design of

sustained-release matrix systems for a highly water-soluble compound, ABT-089. Int. J. Pharmaceutics 157: 43-52, 1997.

94. Predergast, M.A., Jackson, W.J., Terry, Jr., A.V., Decker, M.W., Arneric, S.P. and Buccafusco,

J.J., Central nicotinic receptor agonists ABT-418, ABT-089 and (-)-nicotine reduce distractibility in young-adult monkeys. Psychopharmacology 136: 50-58, 1998.

95. Predergast, M.A., Jackson, W.J., Terry, Jr., A.V., Nancy J. Kille, Arneric, S.P., Decker, M.W. and

Buccafusco, J.J., Age-related differences in distractibility and response to methylphenidate in monkeys. Cerebral Cortex, 8: 164-172,1998.

96. Bannon, A.W., Decker, M.W., Holladay, M.W., Curzon, P., Donnelly-Roberts, D., Puttfarken, P.S.,

Bitner, R.S., Diaz, A., Dickenson, A.H., Williams, M., and Arneric, S.P., Broad spectrum, non-opioid analgesic activity by selective modulation of neuronal nicotinic acetylcholine receptors, Science 279: 77-80, 1998.

97. Decker, M.W., Bannon, A.W., Buckley, M.J., Kim, D.J.B., Holladay, M.W., Ryther, K.B., Wasicak,

J.T., Williams, M., and Arneric, S.P. Antinociceptive effects of the novel cholinergic channel modulator, ABT-594, in mice. Eur. J. Pharmacol., 346:23-33, 1998.

98. Holladay, M.W., Wasicak, J.T., Lin, Nan-Horng, He, Y., Ryther, K.B., Buckl_ey, M.J., Bannon,

A.W., Kim, D.J.B., Decker, M.W., Anderson, D.J., Campbell, J.E., Kuntzweiler, T.A., Donnelly-Roberts, D.L., McKenna, D.G., Piattoni-Kaplan, M., Niforatos, W.E., Briggs, C.A., Williams, M., and Arneric, S.P., Identification and structure-activity relationships of ABT-594 as a potent, orally active analgesic agent acting via neuronal nicotinic acetylcholine receptors. J. Med. Chem. 41: 407-412, 1998.

99. Donnelly-Roberts, D., Puttfarken, P.S., Kunztweiler, T.A., Briggs, C.A., Anderson, D.J., Campbell,

J.E., Piatonni-Kaplan, M., McKenna, D.G., Wasicak, J.T., Holladay, M.W., Williams, M., and Arneric, S.P., 5-((2R)-azetidinylmethoxy)-2-chloropyridine [ABT-594]: A novel, orally effective antinociceptive agent acting via neuronal nicotinic acetylcholine receptors. I. In vitro characterization. J. Pharmacol. Exp. Therap. 285:777-786, 1998.

100. Bannon, A.W., Decker, M.W., Curzon, P., Buckley, M.J., Kim, D.B.J., Lynch, J.K., Wasicak, J.T.,

Arnold, W.H., Holladay, M.W., and Arneric, S.P., 5-((2R)-azetidinylmethoxy)-2-chloropyridine [ABT-594]: A novel, orally effective antinociceptive agent acting via neuronal nicotinic acetylcholine receptors. II. In vivo characterization. J. Pharmacol. Exp. Therap. 286: 787-794, 1998.

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101. Holladay, M.W., Bai, H., Li, Y., Lin, N-H., Daanen, J., Ryther, K.B., Wasicak, J., Kincaid, J.F., He, Y., Hettinger, A.M, Huang, P., Anderson, D.J., Bannon, A.W., Buckley, W.J., Campbell, J.E., Donnelly-Roberts, D., Gunther, K., Kim, D.J., Kuntzweiler, T.A., Sullivan, J.P., Decker, M.W. , Arneric, S.P. Stucture-activity studies related to ABT-594, a potent non-opioid analgesic agent: Effect of pyridine and azetidine ring substitutions on nicotinic acetylcholine receptor binding affinity and analgesic activity in mice. Bioorg. Med. Chem. Lett. 8: 2797-2802, 1998.

102. Curzon, P., Nikkel, A.L., Bannon, A.W., Arneric, S.P., and Decker, M.W., Differences between

the antinociceptive effects of the cholinergic channel activator A-85380 and (+)-epibatidine in rats, J. Pharmacol. Exp. Therap. 287: 847-853, 1998.

103. Sullivan, J.P., Anderson, D.J., Raszkiewicz, J. Campbell, J.E., Hettinger, A.M., Garvey, D.S., and

Arneric, S.P., Receptor binding properties of [3H]A-85380: A high affinity radioligand binding to neuronal nicotinic acetylcholine receptor subunits. Eur. J. Pharmacol. (In preparation), 1998.

104. Bitner, R.S., Nikkel, A.L., Curzon, P., Arneric, S.P., Bannon, A.W., Decker, M.W., Role of the

nucleus raphe magnus in antinociception produced by ABT-594: immediate early gene responses possibly linked to neuronal nicotinic acetylcholine receptors on serotonergic neurons. J. Neurosci., 18:5426-5432, 1998.

105. Curzon, P. Nikkel, A.L., Bannon, A.W., Arneric, S.P., and Decker, M.W., Differences between

the antinociceptive effects of the cholinergic channel activators A-85380 and (+/-)-epibatidine in rats. J Pharmacol Exp Ther. , Dec;287(3):847-53, 1998.

106. Bannon, A.W., Decker, M.W., Kim, D.J.B., Campbell, J.E., and Arneric, S.P., ABT-594, a novel

cholinergic channel modulator, is efficacious in nerve ligation and diabetic neuropathy models of neuropathic pain. Brain Research 801: 158-163, 1998.

107. Decker, M.W., Curzon, P., Holladay, M.W., Nikkel, A.L., Bitner, S.R., Bannon, A.W., Donnelly-

Roberts, D.L., Puttfarken, P.S., Kuntzweiler, T.A., Briggs, C.A., Williams, M., Arneric, S.P., The role of neuronal nicotinic acetylcholine receptors in antinociception: Effects of ABT-594, J. Physiology (Paris), 92:221-224, 1998.

108. Molinari, E.J., Delbono, O., Messi, M.L., Renganathan, M., Arneric, S.P., Sullivan, J.P.,

Gopalakrishnan, M. Up-regulation of human alpha7 nicotinic receptors by chronic treatment with activator and antagonist ligands. Eur. J. Pharmacol. Apr 17;347(1):131-9, 1998.

109. Briggs, C.A., McKenna, D.G., Monteggia, L.M., Touma, E., Roch, J.-M., Arneric, S.P.,

Gopalakrishnan, M., Sullivan, J.P., Gain of function mutation of the nicotinic receptor: distinct

pharmacology of the human V274T variant. Eur. J. Pharmacol. 366:301-308, 1999.

110. Lin, N.H., Abreo, M.A., Gunn, D.E., Lebold, SA, Lee, E.L., Wasicak, J.T., Hettinger, A.M., Daanen, J.F., Garvey, D.S., Campbell, J.E., Sullivan, J.P., Williams, M., and Arneric, S.P., Structure-activity studies on a novel series of cholinergic channel activators based on a heteroaryl ether framework. Bioorg. Med. Chem. Lett. 9(18): 2747-2752, 1999.

111. Seiffert, D., Bradley, J.D., Rominger, C.M., Rominger, D.H., Yang, F., Meredith, J.E., Wang, Q.,

Roach, A.H., Thompson, L.A., Spitz, S.M., Higaki, J.N., Prakash, S.R., Combs, A.P., Copeland, R.A., Arneric, S.P., Hartig, P.R., Robertson, D.W., Cordell, B, Stern, A.M., Olson, R.E., and Zaczek, R., Presenilin-1 and –2 are molecular targets for gamma-secretase inhibitors. J. Biol. Chem. 275(44): 34086-91, 2000.

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112. Ho, S.P., Takahashi, L.K., Livanov, V., Spencer, K., Lesher, T., Maciag, C., Smith, M.A., Rohrbach, K.W., Hartig, P.R., and Arneric, S.P., Attenuation of fear conditioning by antisense inhibition of brain corticotropin releasing factor-2 receptor. Brain Res Mol Brain Res. Apr 18;89(1-2):29-40, 2001.

113. Takahashi, L.K., Ho, S.P., Livanov, V., Graciani, N., and Arneric, S.P. Antagonism of CRF(2) receptors produces anxiolytic behaviors in animal models of anxiety. Brain Res. 902: 135-142, 2001.

114. Schroder, H., Schutz, U., Burghaus, L., Lindstrom, J., Kuryatov, A., Monteggia, L., deVos, R.A.I.,

van Noort, G., Wevers, A., Nowacki, S., Happich, E., Moser, N., Arneric, S.P., Maelicke, A.,

Expression of the 4 isoform of the nicotinic acetylcholine receptor in the fetal human cerebral cortex. Developmental Brain Research. 132: 33-45, 2001.

115. Lin, N.H., Li, Y., He, Y., Holladay, M.W., Kuntzweiler, T. Anderson, D.J., Campbell, J.E. and Arneric, S.P., Synthesis and structure-activity relationships of 5-substituted pyridine analogues. Bioorg. Med. Chem. Lett. 11(5): 631-633, 2001.

116. Arvanitis, A.G., Rescintino, J.T., Arnold, C.R., Wilde, R.G., Cain, G.A., Sun, J.H., Yan, J-S.,

Teleha, C.A., Fitzgerald, McElroy, J., L.W., Zaczek, R., Hartig, P.R., Grossman, S., Arneric, S.P., Gilligan, P.J., Olson, R.E., and Robertson, D.W. , Imidazo[4,5b]pyridines as corticotropin releasing factor receptor ligands. Biorganic & Medicinal Chemistry Letters 13: 125-128, 2003

117. Arvanitis, A.G., Rescintino, J.T., Arnold, C.R., Wilde, R.G., Fitzgerald, L.W., Zaczek, R., Hartig, P.R., Grossman, S., Arneric, S.P., Gilligan, P.J., Olson, R.E., and Robertson, D.W. , Imidazo[4,5c]pyridines as corticotropin releasing factor receptor ligands. Biorganic & Medicinal Chemistry Letters 13: 129-131, 2003.

118. Bain, J.N., Prendergast, M.A., Terry, A.V .Jr., Arneric, S.P., Smith, M.A., Buccafusco, J.J.,

Enhanced attention in rhesus monkeys as a common factor for the cognitive effects of drugs with abuse potential. Psychopharmacology (Berl). Sep;169(2):150-60, 2003.

119. Lelas, S,, Wong, H., Li, Y.W., Heman, K.L., Ward, K.A., Zeller, K.L., Sieracki, K.K., Polino, J.L., Godonis, H.E., Ren, S.X., Yan, X.X., Arneric, S.P., Robertson, D.W., Hartig, P.R., Grossman, S., Trainor, G.L., Taub, R.A., Zaczek, R., Gilligan, P.J., McElroy, J.F. Anxiolytic-like Effects of the CRF1 Antagonist DMP904 Administered Acutely or Chronically at Doses Occupying Central CRF1 Receptors in Rats. J Pharmacol Exp Ther. 309(1), 293-302, 2004.

120. Hurst, R.S., Hajos, M., Raggenbass, M., Wall, T.M., Higdon, N.R., Lawson, J.A., Rutherford-Root, K.L., Berkenpas, M.B., Hoffmann, W.E., Piotrowski, D.W., Groppi, V.E., Allaman, G. Ogier, R., Bertrand, S., Bertrand, D., Arneric, S.P., Novel Positive Allosteric Modulator of the {alpha}7 Neuronal Nicotinic Acetylcholine Receptor: In Vitro and In Vivo Characterization ,J. Neurosci. 25 4396-4405, 2005.

121. Wishka, D.G., Walker, D.P., Yates, K.M., Reitz, S.C., Jia, S., Myers, J.K., Olson, K.L., Jacobsen,

E.J., Wolfe, M.L., Groppi, V.E., Hanchar, A.J., Thornburgh, B.A., Cortes-Burgos L.A., Wong, E.H., Staton, B.A., Raub, T.J., Higdon, N.R., Wall, T.M., Hurst, R.S., Walters, R.R., Hoffmann, W.E., Hajos, M., Franklin, S., Carey, G., Gold, L.H., Cook, K.K., Sands, S.B., Zhao, S.X., Soglia, J.R., Kalgutkar, A.S., Arneric, S.P., Rogers, B.N., Discovery of N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an agonist of the alpha7 nicotinic acetylcholine receptor, for the potential treatment of cognitive deficits in schizophrenia: synthesis and structure--activity relationship. J Med Chem. 2006 Jul 13;49(14):4425-36.

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122. Gilligan, P.J., He, L., Clarke, T., Tivitmahaisoon, P., Lelas, S., Li, Y-W., Heman, K., Fitzgerald, L., Miller, K., Zhang, G., Marshall, A., Krause, C., McElroy, J., Ward, K., Shen, H., Wong, H., Grossman, S., Nemeth, G., Zaczek, R., Arneric, S., Hartig, P., Robertson, D., Trainor, G., 8-(4-Methoxyphenyl)-pyrazolo-[1,5-a]-1,3,5-triazines: Selective and centrally active corticotropin-releasing factor receptor-1 (CRF1) antagonists. J. Med. Chem., 2009 May 14;52(9):3073-83.

123. Gilligan, P.J., Clarke, T., He, L., Lelas, S., Li, Y.W., Heman, K., Fitzgerald, L., Miller, K., Zhang, G., Marshall, A., Krause, C., McElroy, J.F., Ward, K., Zeller, K., Wong, H., Bai, S., Saye, J., Grossman, S., Zaczek, R., Arneric, S.P., Hartig P,, Robertson, D., Trainor, G.

Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists. J Med Chem. 2009 May 14;52(9):3084-92.

124. Belardetti, F., Tringham, E., Eduljee, C., Jiang, X., Dong, H., Hendrickson, A., Shimizu, Y., Janke, D.L., Parker, D., Mezeyova, J., Khawaja, A., Pajouhesh, H., Fraser, R.A., Arneric, S.P., Snutch, T.P. A fluorescence-based high-throughput screening assay for the identification of T-type calcium channel blockers. Assay Drug Dev Technol. 2009 Jun;7(3):266-80.

125. Buccafusco , J.J., Terry, A.V. Jr., Vazdarjanova, A., Snutch, T.P., Arneric, S.P. Treatments for neuropathic pain differentially affect delayed matching accuracy by macaques: effects of amitriptyline and gabapentin. Pain. 2010 Mar;148(3):446-53.

126. Abbadie, C. , McManus, O.B., Sun, S.Y., Bugianesi, R.M., Dai, G., Haedo, R.J., Herrington, J.B., Kaczorowski, G.J., Smith, M.M., Swensen, A.M., Warren, V.A., Williams, B., Arneric, S.P., Eduljee, C., Snutch, T.P., Tringham, E.W., Jochnowitz, N., Liang, A., Euan, MacIntyre, D., McGowan, E., Mistry, S., White, V.V., Hoyt, S.B., London, C., Lyons, K.A., Bunting, P.B., Volksdorf S, Duffy JL. Analgesic effects of a substituted N-triazole oxindole (TROX-1), a state dependent,voltage-gated calcium channel 2 blocker. J Pharmacol Exp Ther. Aug;334(2):545-55, 2010.

127. Hildebrand, M.E., Smith, P., Bladen, C., Eduljee, C., Xie, J.Y., Chen, L., Fee-Maki, M., Doering, C.J., Mezeyova, J., Zhu, Y., Belardetti, F., Pajouhesh, H., Arneric, S.P., Parker, D.P., Parmar, M., Porreca, F., Tringham, E., Zamponi, G.F., Snutch, T.P., A novel slow inactivation specific ion channel modulator attenuates neuropathic pain. Pain (2011)152:833-43.

128. Swensen, A.M., Herrington, J., Bugianesi, R.M., Dai, G., Haedo, R.J., Ratliff, K.S., Smith, M.M., Warren, V.A., Arneric, S.P., Eduljee, C., Parker, D., Snutch, T.P., Hoyt, S.B., London, C., Duffy, J.L., Kaczorowski, G.J., McManus, O.B., Characterization of the Substituted N-Triazole Oxindole TROX-1, a Small-Molecule, State-Dependent Inhibitor of Cav2 Calcium Channels. Molecular Pharmacology March 81(3): 488-497, 2012.

REVIEWS 1. Arneric, S.P., International symposium on nicotine: The effects of nicotine on biological systems

II, Meetings Reports CNS, 3:7-11, 1994. 2. Decker, M.W., Brioni, J.D., Bannon, A.W., and Arneric, S.P., Diversity of neuronal nicotinic

acetylcholine receptors: Lessons from behavior and implications for CNS therapeutics, Life Sci. 56: 545-570, 1995.

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3. Arneric, S.P., Sullivan, J.P., Decker, M.W., Brioni, J.D., Bannon, A.W., Briggs, C.A., Donnelly-Roberts, D., Marsh, K.C., Kyncl, J., Williams, M., and Buccafusco, J.J., Potential treatment of Alzheimer's disease using cholinergic channel activators (ChCAs) with cognition enhancement, anxiolytic-like and cytoprotective properties. Alzheimer's Diseases & Associated Disorders 9:50-61, 1995.

4. Sullivan, J.P., Decker, M.W., Donnelly-Roberts, D., Brioni, J.D., Bannon, A.W., Holladay, M.W.,

Briggs, C.A., Williams, M., and Arneric, S.P., Cholinergic channel activators: Novel opportunities for the treatment of CNS disorders. Proceedings Western Pharmacol. Soc. 38: 127-130, 1995.

5. Arneric, S.P., Sullivan, J.P., Briggs, C.A., Donnelly-Roberts, D., Decker, M.W., Brioni, J.D.,

Marsh, K.C., and Rodrigues, A.D. Preclinical pharmacology of ABT-418: A prototypical cholinergic channel activator for the potential treatment of Alzheimer's disease CNS Drug Rev. 1: 1-26, 1995.

6. Arneric, S.P., Holladay, M.W., and Sullivan, J.P., Cholinergic channel modulators as a novel

therapeutic strategy for Alzheimer's disease. Exp. Opin. Invest. Drugs 5(1): 79-100, 1996. 7. Williams, M. and Arneric, S.P., Beyond the tobacco debate: dissecting out the therapeutic

potential of nicotine. Exp. Opin. Invest. Drugs 5(8): 1035-1045, 1996. 8. Arneric, S.P., Sullivan, J.P., and Williams, M., Fourth International Nice/Springfield Symposium

on Advances for Alzheimer's therapy, Nice, France, April 10-14, 1996, Alzheimer's disease ID research alert 1(1): 7-13, 1996.

9. Brioni, J.D., Morgan, S.J., O'Neill, A.B., Sykora, T.M., Postl, S.P., Pan, J.B., Sullivan, J.P., and

Arneric, S.P. In vivo profile of novel nicotinic ligands with CNS selectivity. Med. Chem. Res. 1996: 487-510, 1996.

10. Holladay, M.W., Lin, N.H., Sullivan, J.P., Donnelly-Roberts, D., Ferrero, J., Rodrigues, A.D.,

Marsh, K.C., Decker, M.W., Brioni, J.D., Buccafusco, J.J, and Arneric, S.P., Progress in the development of potent and selective cholinergic channel modulators. Proc. XIVth International Symp. on Med. Chem. pp. 127-136, 1997.

11. Kowaluk, E.A., Arneric, S.P., and Williams, M., Opportunities in pain therapy: Beyond the

opioids and NSAIDs. Emerging Drugs 3: 1-37, 1998. 12. Kowaluk, E.A. and Arneric, S.P., Novel molecular approaches to analgesia, Annual Reviews in

Medicinal Chemistry, 33: 11-20, 1998. 13. Williams, M., Kowaluk, E.A., and Arneric, S.P., Emerging molecular approaches to pain therapy.

J. Med. Chem. May 6;42(9):1481-500, 1999. 14. Arneric, S.P., Holladay, M.W., and William, M., Neuronal nicotinic receptors: a perspective on

two decades of drug discovery research, Biochem. Pharmacol. 74(8): 1032-1101, 2007.

15. Stephenson, D. and Arneric, S.P., Neuroimaging of Pain: Advances and Future Prospects, J.Pain, 2008 Jul;9(7):567-79.

16. Zamponi, G.W., Lewis, R.L., Todorovic, S.M., Arneric, S.P., Snutch, T.P., Role of calcium channels in ascending pain pathway. Brain Research Reviews Apr 60(1): 84-89, 2009.

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17. Knopp KL, Nisenbaum ES & Arneric, S.P. Evolving Cancer Pain Treatments: Rational Approaches To Improve the Quality of Life for Cancer Patients. Current Pharmaceutical Biotech. Oct;12(10):1627-43, 2011.

18. Arneric, S.P., Kennedy, J.D., Laird, J., & Chappell, A.S., Tailoring Chronic Pain Treatments for the Elderly: Are We Prepared for the Challenge? Drug Discovery Today, Jan 19(1): 8-17, 2014.

BOOKS EDITED 1. Neuronal Nicotinic Receptors: Pharmacology and Therapeutic Opportunities (eds. S.P. Arneric

and J.D. Brioni), Wiley Press, New York, NY, 1999. BOOK CHAPTERS 1. Downen, M., Sugaya,K., Arneric, S.P. , and Giacobini, E. Presynaptic markers of cholinergic

function in cortex following ibotenic acid lesion of basal forebrain. In: Novel Treatments and Models For Alzheimer's Disease (eds. E.M. Meyer, J. Simpkins and J. Yamamoto) Plenum Press, NY, 1989.

2. Arneric, S.P. New nicotinic agonists and cerebral blood flow, In: Second International Springfield

Alzheimer Symposium, May 3-5, 1991, Springfield, IL (eds. E. Giacobini, and R. Becker), Birkhauser Boston Inc. pp. 386-394, 1991.

3. Arneric, S.P. and Williams M., Nicotinic agonists in Alzheimer's disease: Does the

molecular diversity of nicotine receptors offer the opportunity for developing CNS selective cholinergic channel activators? In Racagni G., Brunello N., Langer S.Z. (eds.): Recent Advances In The Treatment of Neurodegenerative Disorders and Cognitive Funcition, Int. Acad. Biomed. Drug Res., Basel, Karger, vol. 7, pp. 58-70, 1994.

4. Williams, M., Sullivan, J.P., and Arneric, S.P., Neuronal nicotinic acetylcholine receptor:

Molecular advances and therapeutic opportunities, In: Drug News and Perspectives, (eds. Prose), Vol. 7 (4):205-223, 1994.

5. Arneric, S.P., Sullivan, J.P., Decker, M.W., Brioni, J.D., Buccafusco, J.J., Briggs, C.A., Marsh,

K., Rodrigues, A.D., Donnelly-Roberts, Garvey,D.S., and Williams, M. ABT- 418: A novel cholinergic channel activator for the treatment of Alzheimer's disease, In: Alzheimer Disease: Therapeutic Strategies, (eds. E. Giacobini, and R. Becker), Birkhauser Boston Inc. , pp.196-200, 1994

6. Raszkiewicz, J.L., Sullivan, J.P. and Arneric, S.P., Effect of cholinergic enhancers on basal

forebrain function governing cortical cerebral blood flow. In: Alzheimer's and Parkinson's Diseases, Plenum Press, New York, pp. 251-257, 1995.

7. Arneric, S.P., Sullivan, J.P., and Williams, M. Neuronal nicotinic acetylcholine receptors: novel

targets for CNS therapeutics. In: Psychopharmacology: 4th Generation of Progress (eds. F.E. Bloom and D.J. Kupfer), Raven Press, New York , pp. 94-110, 1995.

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8. Bannon, A.W., Decker, M.W., Williams, M. and Arneric, S.P., Psychotherapeutic potential of selective neuronal nicotinic acetylcholine receptor ligands. In: Brain Imaging of Nicotine and Tobacco Smoking (ed. E. Domino), NPP Books, P.O. Box 1491, Ann Arbor, MI, 48106, pp. 1-23, 1995.

9. Williams, M, Sullivan, J.P., Bannon, A.W. and Arneric, S.P., Selective neuronal nicotinic

acetylcholine receptor ligands: A novel class of CNS therapeutic agents, Massachusetts General Hospital Psychopharmacology ,Winter Conference Series, 1995.

10. Arneric, S.P., Bannon, A.W., Briggs, C.A, Brioni, J.D., Buccafusco, J.J., Decker, M.W.,

Gopalakrishnan, M., Holladay, M.W., Kyncl, J., Lin, N.H., Marsh, K.G., Qiu, Y.H., Radek, R., Donnelly-Roberts, D.L., Sullivan, J.P. and Williams, M. ABT-089: an orally active cholinergic channel modulator (ChCM) with cognition enhancing and neuroprotective activity In: Alzheimer Disease: From Molecular Biology to Therapy, (eds. R. Becker E. Giacobini, and P. Robert), Birkhauser Boston Inc., pp.287-292, 1996.

11. Williams, M. and Arneric, S.P., Alzheimer's disease: Prospects for treatment in the next decade.

In: Alzheimer's Disease (eds. J. D. Brioni and M.W. Decker, Wiley-Liss, New York, 1996. 12. Brioni, J.D., Decker, M.W., Sullivan, J.P., and Arneric, S.P., The Pharmacology of (-)-Nicotine

and Novel Cholinergic Channel Modulators. In: Advances in Pharmacology, Vol. 37 (eds. J.T. August, M.W. Anders, F. Murad, J.T. Coyle) Academic Press, San Diego, pp. 153-214, 1997.

13. Arneric, S.P., Neurobiology of neuronal nicotinic acetylcholine receptors. In: Nicotine:

Psychotropic and Psychotropic Effects. (eds. M. Piasecki and P. Newhouse), American Psychiatric Press, Inc., Washington D.C., 1998.

14. Decker, M.W. and Arneric, S.P., Nicotinic acetylcholine receptor - targeted compounds: a

summary of the development pipeline and therapeutic potential. In: Neuronal Nicotinic Receptors: Pharmacology and Therapeutic Opportunities (eds. S.P. Arneric and J.D. Brioni), Wiley, New York, 1999.

15. Arneric, S.P. and Holladay, M.W, Agonists and antagonists of nicotinic acetylcholine receptors.

In: Handbook of Experimental Pharmacology "Neuronal Nicotinic Receptors", (eds F. Clementi, C. Gotti, and D. Fornasari) Springer-Verlag, Heidelberg, 1999.

16. Arneric, S.P. Cholinergic approaches to treat pain. In: Pain: Current Understanding, Emerging Therapies and Novel Approaches to Drug Discovery. (eds. C. Bountra, R. Munglani, W.K. Schmidt ) Marcel Dekker, New York, 2003. pp. 749-762.

17. Arneric, S.P. and Sher, E., Current & Future Trends in Drug Discovery and Development Related to Nicotinic Receptors, In: Nicotine Receptors (edited by Dr. Robin Lester and Dr. Paul Kenny), 2014 (In Press).

ABSTRACTS PUBLISHED 1. Arneric, S.P., McCormack, K.M. and Hook, J.B. Altered progesterone metabolism following

polybrominated biphenyls (PBBs). The Pharmacologist 21:383, 1979. 2. Arneric, S.P., Goodale, D.B., Flynn, J.R. and Long, J.P. Simultaneous DOPA and 5-HTP

analysis from rat brain utilizing HPLC with electrochemical detection. Soc. for Neurosci. 6:235, 1980.

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3. Arneric, S.P., Goodale, D.B., Flynn, J.R., Long, J.P., Barfknecht, C.F. and Cannon, J.G. Altered

dopamine and serotonin biosynthesis in CNS following rigid congeners of amphetamine. The Pharmacologist 22:147, 1980.

4. Maixner, W., Arneric, S.P., Lecompte, J., Verimer, T., Cannon, J.G., Lee, T. and Long, J.P.

Pharmacological properties of 2-aminotetralins, octahydro-benoz(f)quinolines and clonidine on the isolated guinea pig ileum. The Pharmacologist 22:48, 1980.

5. Walsh, B.J., Goodale, D.B., Long, J.P., Arneric, S.P. and Flynn, J.R. Inhibition of rotational

behavior by haloperidol, metoclopramide, pimozide and sulpiride. The Pharmacologist 22:145, 1980.

6. Verimer, T., Long, J.P., Koble, D.L., Cannon, J.G., Flynn, J.R., Goodale, D.B. and Arneric, S.P.

Effects of 5-hydroxy-6-methyl-2-aminotetralin derivatives on pre- and postsynaptic dopaminergic receptors. The Pharmacologist 22:760, 1980.

7. Arneric, S.P., Goodale, D.J., Long, J.P., Gebhart, G.F., Lakoski, J.M., Mott, J. and Barfknecht,

C.F. RDS-127: A potent nonhydroxylated dopamine agonist. Soc. for Neurosci. 7:34.6, 1981. 8. Arneric, S.P., Collins, E.D., Bhatnagar, R.K. and Long, J.P. Is domperidone a selective

peripheral dopamine receptor antagonist? Fed. Proc. 41:4639, 1982. 9. Arneric, S.P., Chow, S., Webb, R.L., Bhatnagar, R.K., Long, J.P. and Fischer, L.J. Evidence for

central pathways mediating the hyperglycemia produced by dopamine-receptor agonists in the rat. Soc. for Neurosci. 8:421, 1982.

10. Arneric, S.P., Chow, S.A., Long, J.P. and Fischer, L.J. Dopamine analogs inhibit insulin release

from isolated pancreatic islets. Fed. Proc. 42:2060, 1983. 11. Chow, S.A., Arneric, S.P., Fischer, L.J. and Long, J.P. Dopamine-agonist induced alterations in

insulin secretion and blood glucose. Fed. Proc, 41:4637, 1982. 12. Long, J.P., Bhatnagar, R.K., Arneric, S.P. and Cannon, J.G. Structure-activity relationships of

presynaptic dopamine agents. 1982. 13. Arneric, S.P. and Long, J.P. RDS-127 (2-di-n-propylamino- 4,7-dimethoxyindane): central

cardiovascular effects of a novel dopamine agonist. The Pharmacologist 25:729, 1983. 14. Arneric, S.P. and Long, J.P. Sympatho-adrenal activation may be modulated by postsynaptic

(D2) dopamine receptors in the hindbrain. Soc. for Neurosci. 9(2):33.2, 1983. 15. Arneric, S.P., Meeley, M.P. and Reis, D.J. Intrinsic cortical peptides modify release of

acetylcholine and neurotransmitter amino acids from brain slices. Fed. Proc. 43, 1984. 16. Arneric, S.P., Meeley, M.P. and Reis, D.J. Somatostatin and cholecystokinin octapeptide

modulate the release of acetylcholine and neurotransmitter amino acids from rat caudate nucleus slices by different mechanisms. Soc. for Neurosci. 1O(1):160.6, 1984.

17. Iwata, J., LeDoux, J.E., Arneric, S.P.`, Meeley, M.P. and Reis, D.J. Auditory fear conditioning is

mediated by projections from the medial geniculate to, not through, an archi-neostriatal field. Soc. for Neurosci. 10(1) 38.8, 1984.

Stephen P. Arneric, Ph.D. – April, 2015 27

18. Arneric, S.P., Iadecola, C., Underwood, M., Ishitsuka, T. and Reis, D.J. Evidence for local cholinergic mechanisms mediating cerebral cortical vasodilation elicited by electrical stimulation of the fastigial nucleus in rat. Fifth Annual Chemical Defence Bioscience Review, 1985.

19. Iadecola, C., Arneric, S.P. and Reis, D.J. Evidence for intrinsic cortical neurons mediating

cerebral cortical vasodilation elicited by electrical stimulation of the rat fastigial nucleus. 12th Symposium on Cerebral Blood Flow and Metabolism. 5 (Suppl. 1):S519, 1985.

20. Arneric, S.P., Meeley, M.P., Honig, M.A. and Reis, D.J. Receptor mediated, Ca2+-dependent

release of tyrosine from brain slices by m-enkephalin and other neuropeptides. Soc. for Neurosci. 11:104.6, 1985.

21. Arneric, S.P., Iadecola, C., Underwood, M.D. and Reis, D.J. Intrinsic neurons mediate the

cortical cholinergic cerebrovasodilation elicited by electrical stimulation of fastigial nucleus (FN). The Pharmacologist 27:574, 1985.

22. Woo, J.I., Saji, M., Arneric, S.P. and Reis, D.J. Neurochemical correlates of transneuronal cell

loss of dopaminergic neurons of substantia nigra. Soc. for Neurosci. 11:365.8, 1985. 23. Reis, D.J., Iadecola, C., Arneric, S.P., Tucker, L.W. and Baker, H. Local proliferation of

capillaries associated with glial cell activation in ibotenic acid lesions of the primary sensory cortex in rat. Soc. for Neurosci. 11:75.27, 1985.

24. Iadecola, C., Arneric, S., Tucker, L.W., Baker, H. and Reis, D.J. Cerebral cortical neurons are

required for the cortical cerebrovasodilation elicited by stimulation of the fastigial nucleus in rat. Soc. for Neurosci. 11:61.23, 1985.

25. Arneric, S.P., Meeley, M.P. and Reis, D.J. Receptor-mediated tyrosine release: A novel

neurotransmitter role? Soc. for Neurochem. 17(1):191, 1986. 26. Arneric, S.P., Giuliano, R., Ernsberger, P., Underwood, M.D. and Reis, D.J. Does acetylcholine

released within the C1 area of the rostral ventrolateral medulla (RVL) tonically maintain arterial pressure? Fed. Proc. 45:3422, 1986.

27. Arneric, S.P., Iadecola, C., Honig, M.A., Meeley, M.P. and Reis, D.J. Acetylcholine is

synthesized and released by elements associated with cerebrocortical microvessels. Soc. for Neurosci. 12:143.11, 1986.

28. Iadecola, C., Arneric, S.P., Baker, H., Callaway, J.L. and Reis, D.J. Non- neuronal cells

contribute to local cerebral blood flow regulation after acute neuronal injury. Neurology 36 (Suppl. 1):228, 1986.

29. Reis, D.J., Arneric, S.P., Underwood. M.D., Goadsby, P.J. and Iadecola, C. Local release of

acetylcholine may mediate the cortical cerebrovasodilation elicited by electrical stimulation of the fastigial nucleus in rat. Soc. for Neurosci. 12:143.12, 1986.

30. Arneric, S.P., Honig, M.A., Milner, T.A., Greco, S., Iadecola, C. and Reis, D.J. Sites of

acetylcholine synthesis and release associated with microvessels in cerebral cortex: ultrastructural and neurochemical studies. J. Cerebral Blood Flow and Metabolism, Vol. 7 (Suppl. 1):S330, 1987.

31. Arneric, S.P. Cholinergic drugs increase cerebral cortical microvascular perfusion (CCMP) via

local muscarinic mechanism. The Pharmacologist 29:412, 1987.

Stephen P. Arneric, Ph.D. – April, 2015 28

32. Arneric, S.P., Ernsberger, P.M., May. A.M., Cheng, P.-Y. and Reis, D.J. Specific, reversible and stereoselective binding of 3H-L-tyrosine to rat forebrain (P2) membranes. Soc. for Neurosci. 13:249.15, 1987.

33. May, A.M. and Arneric, S.P. Effects of basal forebrain lesions and cholinomimetics on cerebral

cortical microvascular perfusion (CCMP) in rat: continuous measurement by laser- doppler flowmetry. Soc. for Neurosci. 13:288.12, 1987.

34. Iadecola, C., Arneric, S.P., Underwood, M.D., Baker, H.D., Callaway, J. and Reis, D.J. Non-

neuronal cells participate in regulating local cerebral perfusion after neuronal death by excitotoxins. Soc. for Neurosci. 13:7.11, 1987.

35. Arneric, S.P. Cortical cerebral blood flow (CBF) is increased by electrical stimulation of the basal

forebrain (BF): Modulation by cholinergic mechanisms. Soc. for Neurosci. 14:488.2, 1988. 36. Cline, W.H., May, A.M., Stephenson, L.L., Kelley, C.R. and Arneric, S.P. Cholinergic,

glutamatergic and noradrenergic transmission in the rostral ventrolateral medulla (RVL) of Wistar Kyoto rats (WKY) and spontaneously hypertensive rats (SHR). Soc. for Neurosci. 14:250.1, 1988.

37. Arneric, S.P. Cholinergic mechanisms regulating cortical cerebral blood flow: role of the basal

forebrain. Alzheimer's Disease Research Workshop, Tucson, Arizona, 1989. 38. Arneric, S.P. Basal forebrain neurons modulate cortical cerebral blood flow: increses by nicotinic

cholinergic mechanisms. J. Cerebral Blood Flow and Metabolism 9 (Suppl. 1):S 502, 1989.

39. Arneric, S.P., Kelley, C.R. and Tingley, F.D. Release of 3H-ACh and endogenous glutamate in rostral ventrolateral medulla (RVL): effects of clonidine. FASEB J. 3(3):A232, 1989.

40. Stephenson, L.L., Cline, W.H. and Arneric, S.P. Noradrenergic transmission in the nucleus

tractus solitarius (NTS), rostral ventrolateral medulla (RVL) and caudal ventrolateral medulla (CVM) of normotensive Wistar Kyoto rats (WKY) and spontaneously hypertensive (SHR). FASEB J. 3(3):A408, 1989.

41. Downen, M., Sugaya, K., Arneric, S.P. and Giacobini, E. Synthesis, release and binding of ACh

in rat cortex following BF lesions. Soc. for Neurochem., 1989. 42. Arneric, S.P. Cortical cerebral blood flow is modulated by cholinergic basal forebrain neurons:

effects of ibotenic acid lesions and electrical stimulation. Satellite Symposium entitled Neurotransmission and Cerebrovascular Function, La Napoule, France, June, 1989.

43. Raza, A. and Arneric, S.P. Selective loss of GABA neurotransmission in the inferior colliculus of

aged Fischer-344 rats. Soc. for Neurosci. 15:445.6 1989. 44. Linville, D. and Arneric, S.P. Basal forebrain (BF)-elicited increases in cortical cerebral blood

flow (CBF): selective age-related impairments. Soc. for Neurosci. 15:17.5, 1989 45. Arneric, S.P., Kelley, C.R., Tingley, F.D., Luthin, D. and Cline, W. Excitatory amino acid (EAA)

transmission in rostral ventrolateral medulla (RVL): EAA antagonists as potential centrally acting antihypertensives? Soc. for Neurosci. 15:385.3, 1989.

46. Faingold, C.L., Arneric, S.P., Randall, M.E. and Copley, C.A. Increased GABA levels or

decreased glutamate (Glu) levels in inferior colliculus (IC) block audiogenic seizure (AGS) susceptibility in genetically epilepsy-prone rats (GEPRs). Soc. for Neurosci. 15:24.1, 1989.

Stephen P. Arneric, Ph.D. – April, 2015 29

47. Downen, M., Sugaya, K., Arneric, S.P. and Giacobini, E. Cortical cholinergic function after basal forebrain lesion. Soc. for Neurosci. 15:165.5, 1989.

48. Arneric, S.P. and Linville, D.G. Selective, age-related impairment of basal forebrain-elicited

increases in cortical cerebral blood flow. Neurobiol. Aging 11: 73 , 1990. 49. Linville, D.G., Arneric, S.P. and Giacobini, E. Basal forebrain-elicited increases in cortical

cerebral blood flow: enhancement by heptyl-physostigmine (Heptastigmine, MF-201), The Basal Forebrain: Anatomy to Function Conference, May 1990.

50. Anderson, D., Cadman, E., Vella-Rountree, L., Arneric, S.P. and Williams, M. The

aminopyridazine muscarinic agonist, SR 95639A, is a functional M2 receptor antagonist in rat brain. Soc. for Neurosci. 16:435.6, 1990.

51. Somani, S.M., Babu, S.R., Arneric, S.P., Dube, S.N. and Manyan, B. Effect of Physostigmine

and exercise on cholineacetyltransferase and acetylcholinesterase activities in brain regions of rat. Soc. for Neurosci. 16:434.7, 1990.

52. Linville, D.G. and Arneric, S.P. Localization of nicotine-induced increases in cortical cerebral

blood flow (CBF). Soc. for Neurosci. 16: 129.9, 1990. 53. Raza, A., Caspary, D.M., and Arneric, S.P. Age-related changes in GABA and ACh in the

brainstem auditory nuclei of Fischer-344 rats. Soc. for Neurosci. 16: 298.3, 1990. 54. Arneric, S.P., Linville, D.G., Kerwin, Jr., J.F., and Murad, F. Nitric oxide (NO): Its role in

mediating increases in cortical cerebral blood flow (CBF) elicited by electrical stimulation of the basal forebrain (BF). Soc. for Neurosci. 16:129.11, 1990.

55. Linville, D.G., and Arneric, S.P. Basal forebrain control of cortical cerebral circulation by nicotinic

mechanisms is independent of local cortical neurons. J. Cerebral Blood Flow & Metabolism, Vol 11(Suppl. 2): S697, 1991.

56. Arneric, S.P., Linville, D.G., Raszkiewicz, J.L., Wagenaar, F. and Kerwin, J.F., Jr., Nitric oxide

(NO) synthase is critical in mediating neurogenic control of the cortical cerebral circulation by the basal forebrain. J. Cerebral Blood Flow & Metabolism, Vol. 11(Suppl. 2): S25, 1991.

57. Linville, D.G., Williams, S., Raszkiewicz, J. and Arneric, S.P. Nicotine receptor agonists

enhance basal forebrain-mediated increases in cortical cerebral blood flow. Second Springfield International Symposium on Alzheimer's & Related Disorders. May 3-5, 1991.

58. Arneric, S.P., Linville, D.G., Williams, S., Raszkiewicz, J. Basal forebrain (BF) regulation of

cortical cerebral blood flow (CBF): Modulation by subtype-selective nicotine receptor agonists. Soc. for Neurosci. 17: 16.5, 1991.

59. Arneric, S.P., Linville, D.G., Williams, S., E. Giacobini , Heptyl-physostigmine

(HEPTASTIGMINE, MF-201) enhances basal forebrain-elicited increases in cortical cerebral blood flow. Second Springfield International Symposium on Alzheimer's & Related Disorders. May 3-5, 1991.

60. Brioni, J.D., Linville, D.G., Cadman, E., Williams, S., Buckley, M., Anderson, D.J., and Arneric,

S.P. Classical nicotinic agonists differentially affect cognition, cortical cerebral blood flow (CBF) and dopamine (DA) release. Soc. for Neurosci. 17: 488.16, 1991.

Stephen P. Arneric, Ph.D. – April, 2015 30

61. Garvey, D.S., Chung, J.Y.-L., Shue, Y.K., Cadman, E., Anderson, D.J., Arneric, S.P., and Williams, M., Novel amino terminally modified derivatives of oxotremorine are more efficacious agonists at cortical muscarinic receptors of the M-1 substype. Soc. for Neurosci. 17:162.1, 1991

62. Linville, D.G., Williams, S., Majchrzak, M.J., Raszkiewicz, J. and Arneric, S.P. Basal forebrain

(BF) regulation of cortical cerebral blood flow (CBF): Effects of aging and chronic nicotine treatment. Soc. for Neurosci. 17: 16.4, 1991

63. Anderson, D.J. and Arneric, S.P. Neuronal nicotinic receptor binding in rat brain: A comparison

of three radioligands. Soc. for Neurosci. 17: 488.16, 1991. 64. Kang, C.H., Nakane, M., Kerwin Jr., J.F., Forstermann, U. and Arneric, S.P. A novel method for

measuring purified nitric oxide (NO)-synthase activity in rat brain: Kinetic correlation of NADP and citrulline formation from L-arginine. Soc. for Neurosci. 17:40.8, 1991.

65. Lin, N-H., Anderson, D.J., Cadman, E., Garvey, D.S. and Arneric, S.P. Synthesis and evaluation

of nicotine analogs as neuronal nicotinic receptor ligands. American Chemical Society, Washington, D.C., Aug. 23-28, 1992.

66. Cadman, E. and Arneric, S.P. Evidence for functional diversity of neuronal nAChRs regulating

neurotransmitter release in rat brain. Cholinergic Neurotransmission: Function and Dysfunction, Montreal, Canada , July 25-30, 1992.

67. Brioni, J. , Curzon, P., Buckley, M.J., Arneric, S.P., and Decker, M.W., DuP996 (Linopirdine)

facilitates the retention of avoidance training and improves performance of septal-lesioned rats in the water maze. Soc. for Neurosci. ,18: 362.10, 1992.

68. Raszkiewicz, J. , Hettinger, A.M., Turek, J.W. and Arneric, S.P. Enhancement of cortical cerebral

blood flow by (+)2-methylpiperidine, a putative allosteric modulator on neuronal nicotinic receptors, Soc. of Neurosci., 18:68.4 , 1992.

69. Buckley, M.J., Decker, M.W. and Arneric, S.P. Effects of nicotinic agonist pretreatment on

nicotine-induced hypothermia and hypolocomotion. Soc. for Neurosci., 18: 42.17 ,1992. 70. Decker, M.W., M.J. Majchrzak and Arneric, S.P., Learning and memory effects of the nicotinic

agonist lobeline in rats, Soc. for Neurosci., 18: 147.24 , 1992. 71. Adams, P., Cheng, H., Kohlhaas, K., Arneric, S.P., and Sullivan, J.P., Modulatory role of nicotine

on NMDA-induced increases in cGMP levels in rat cerebellar slices. Soc. for Neurosci., 18: 337.10 , 1992.

72. Arneric, S.P., Sullivan, J.P., Anderson, D.J., Raszkiewicz, J., Hughs, M.L., C. Briggs, Buckley,

M.J., Decker, M.W., and Hettinger, A.M., D.S. Garvey , (+)2-Methylpiperidine: An allosteric modulator of central neuronal nicotinic receptors, Soc. for Neurosci., 18: 259.5 , 1992.

73. Pan, J.B, Casuto, D., Watanabe, S., Arneric, S.P., and Giordano, T., Neurotrophin induction in

the adult rat brain following administration of thyroid hormone, Soc. for Neurosci., 18: 355.8 , 1992.

74. Monteggia, L, Arneric, S.P. and Giordano, T., Nicotine effects on regulation of APP splicing and

neurotrophin levels in SH-SY5Y cells, Soc. for Neurosci., 18:601.12 , 1992. 75. Anderson, D.J., Raszkiewicz, J.L., and Arneric, S.P., Age-related changes in rat brain neuronal

nicotinic receptors. Soc. for Neurosci., 18: 337.8, 1992.

Stephen P. Arneric, Ph.D. – April, 2015 31

76. Garvey, D.S., Wasicak, J.T., Lin, N.-H., He, Y., Elliott, R., Hettinger, A.M., Anderson, D.J., Raszkiewicz, J.A., Decker, M.W., Brioni, J., Buckley, M.J, Sullivan, J.P., Arneric, S.P. and Williams, M., Novel Ligands for Neuronal Cholinergic Channel Receptors, ACS Meeting, Denver, CO , March 1993.

77. Arneric, S.P., Linville, D.G., Raszkiewicz, J.L. ,Curzon, P., O'Neill, A., Kang, C.H., Turek, J.W.,

Sullivan, J.P., Brioni, J. and Decker, M.W., Nicotinic cognition enhancing agents improve performance by facilitating basal forebrain neurons governing cortical CBF, BRAIN '93, Sendai, Japan, May 1993.

78. Arneric, S.P. and William, M, Nicotinic agonists in Alzheimer's Disease: Does the molecular

diversity of nicotine receptors offer the opportunity for developing CNS selective cholinergic channel activators? Recent Advances In The Treatment of Neurodegenerative Disorders and Cognitive Dysfunction, Capri, Italy, May 1-3, 1993.

79. Kim, D.B.J., Williams, J., O'Neill, A.B., Decker, M.W., Arneric, S.P. and Brioni, J.D., Clozapine

blocks the discriminative stimulus properties of nicotine, Soc. for Neurosci., 19:310.20, 1993. 80. Monteggia, L.M., Sullivan, J.P., Briggs, C.A., Hughes, M.A., Arneric, S.P. Downen, M., Wainer,

B. H. and Giordano, T., Analysis of nicotinic receptor subtyes in immortalized hippocampal and septal fusion cell lines, Soc. for Neurosci., 19:123.11, 1993.

81. Briggs, C.A., Hughes, M.L., Monteggia, L.M., Arneric, S.P., Downen, M., Wainer, B.H. and

Giordano, T., Electrophysiologic evaluation of nicotinic responsiveness in immortalized hippocampal and septal fusion cell lines, Soc. for Neurosci., 19:123.12, 1993.

82. Radek, R.J., Briggs, C., Sullivan, J., Kang, C.H., Arneric, S.P., Effects of subchronic nicotine on

rat EEG, Soc. for Neurosci., 19:377.3, 1993. 83. Brioni, J.D., O'Neill, A.B., Kim, D.B.J., Decker, M.W. and Arneric, S.P., The anxiolytic effect of

nicotinic receptor agonists in the elevated plus-maze test, Soc. for Neurosci., 19310.19, 1993. 84. Kang, C.-H., Raszkiewicz,J.L., Swanson, S., Brioni, J.D., Decker, M.W., Arneric, S.P. and

Sullivan, J.P., Pharmacodynamic and pharmacokinetic studies on erysodine: A potent neuronal nicotinic receptor antagonist, Soc. for Neurosci., 19:631.14, 1993.

85. Sullivan, J.P., Giordano, T., Monteggia, L.M., Downen, M., Wainer, B.H. and Arneric, S.P.,

Cholinergic regulation of intracellular calcium levels in an immortalized hippocampal cell line, Soc. for Neurosci., 19:725.1, 1993.

86. O'Neill, A.B., Brioni, J.D., Buckley, M.J., Kang, C.H., Sullivan, J.P., Raszkiewicz, J.L. Swanson,

S., Arneric, S.P. and Decker, M.W., In vivo characterization of erysodine, an erythrina alkaloid that binds to neuronal nicotinic acetylcholine receptors (nAChRs), Soc. for Neurosci., 19:631.16, 1993.

87. Anderson, D.J., Arneric, S.P., Swanson, S., Raszkiewicz, J.L. and Sullivan, J.P., In vitro

pharmacology of erysodine: A high affinity antagonist of neuronal nicotinic acetylcholine receptors, Soc. for Neurosci., 19:631.15, 1993.

88. Raszkiewicz, J.L., Sullivan, J.P. and Arneric, S.P., Effect of cognition enhancing agents on basal

forebrain-mediated increases in cortical cerebral blood flow (CBF). Third Internation Conf. on Alzheimer's and Parkinson's Diseases, Chicago, IL, Nov. 1-6, 1993

Stephen P. Arneric, Ph.D. – April, 2015 32

89. Arneric, S.P., Decker, M.W., Brioni, J., Sullivan, J.P., Garvey, D.S., Briggs, C., and Williams, M., ABT 418: A novel cholinergic channel activator (ChCA) with cognition enhancing and anxiolytic activity. American College of Neuropsychopharmacology Meeting, Honolulu, Hawaii, Dec. 13th, 1993.

90. Arneric, S.P., Sullivan, J.P., Decker, M.W., Brioni, J.D., Buccafusco, J.J., Briggs, C.A., Donnelly-

Roberts,D. and Williams, M., Cholinergic channel activators (ChCAs) as therapeutics for CNS disorders: ABT 418 [(S)-3-methyl-5-(1-methyl-2-pyrrolidinyl) isoxazole hydrochloride] as a prototype ChCA to treat Alzheimer's disease (AD). XIXth CINP Congress, Washington, D.C., 1994.

91. Decker, M.W., Brioni, J.D., Buckley, M.J., Curzon, and Arneric, S.P., Preclinical cognitive effects

of cholinergic channel ligands. XIXth CINP Congress, Washington, D.C., 1994. 92. Sullivan, J.P., Anderson, D.J., Williams, M., Pauly, J.R., Raszkiewicz, J.L., and Arneric, S.P.,

[3H]ABT 418 [(S)-3-methyl-5-(1-methyl-2-pyrrolidinyl) isoxazole hydrochloride]: Receptor binding properties of a novel cholinergic channel ligand. XIXth CINP Congress, Washington, D.C., 1994.

93. Brioni, J.D., Decker, M.W., Curzon, P., O'Neill, A., Sullivan, J.P., and Arneric, S.P., Cognitive enhancement and anxiolytic-like activity of the novel cholinergic channel activator ABT

418. International Behavioral Neuroscience Soc. Conference. Clearwater Beach, Florida , May 19-22, 1994.

94. Curzon, P., Brioni, J.D., Decker, M.W. and Arneric, S.P., Effect of a novel cholinergic channel

activator, ABT-418, on the acquisition of a spatial discrimination task and locomotor activity in the rat., International Behavioral Neuroscience Soc. Conference. Clearwater Beach, Florida , May 19-22, 1994.

95. Buckley, M.J., Curzon, P., Brioni, J.D., Decker, M.W., Garvey, D.S., Wasicak, J., Williams, M.,

and Arneric, S.P., The effects of ABT-418, a novel cholinergic channel activator, on cognitive function in rodents, Third International Springfield Alzheimer Symposium, May 11-14, 1994, Springfield, IL

96. Arneric, S.P., Sullivan, J.P., Decker, M.W., Brioni, J.D., Buccafusco, J.J., Briggs, C.A., Marsh, K.,

Rodrigues, A.D., Donnelly-Roberts, D., Pauly, J., Garvey, D.S. and Williams, M. Development of novel cholinergic channel activator (ChCA) compounds: A new therapeutic approach for the treatment of CNS disorders, Cholinergic Signalling in Alzheimer's Disease: Therapeutic Strategies, Sept. 4-8, 1994, Vienna, Austria.

97. Garvey, D.S., Wasicak, J.T., Lin, N-H., He, Y., Elliott, R., Hettinger, A-M., Lebold, S., Anderson,

D.J., Cadman, E.D., Raszkiewicz, J.L., Sullivan, J.P., Arneric,S.P., and Williams, M., Isoxazole and isothiazole ligands that interact with neuronal cholinergic channel receptors. 207th ACS National Meeting: Division of Medicinal Chemistry, March 13-17, 1994, San Diego, CA.

98. Radek, R.J., Briggs, C.A., and Arneric, S.P., In vivo electrophysiological effects of ABT-418: a

nov_el cholinergic channel activator. Soc. for Neurosci., 20: , 1994. 99. Anderson, D.J., Campbell, J.E., Kang, C.H., Raszkiewicz, J.L., Arneric, S.P., and Sullivan, J.P.,

The effect of chronic ABT-418 and (-)-nicotine on neuronal nicotinic acetylcholine receptor binding properties in rat brain. Soc. for Neurosci., 20: , 1994.

100. Decker, M.W., Brioni, J.D., Buckley, M.J., Curzon, P., Williams, M., and Arneric, S.P., ABT-418:

A novel cholinergic channel activator with cognitive enhancing properties. Soc. for Neurosci., 20: , 1994.

Stephen P. Arneric, Ph.D. – April, 2015 33

101. Brioni, J.D., O'Neill, A.B., Kim, D.J.B., Decker, M.W., and Arneric, S.P., ABT-418: the anxiolytic and discriminative stimulus properties in rodents. Soc. for Neurosci., 20: , 1994.

102. Sullivan, J.P., Anderson, D.J., Donnelly-Roberts, D., Raszkiewicz, J.L., Williams, M., and

Arneric, S.P., ABT-418 differentially activates putative subtypes of neuronal nicotinic acetylcholine receptors. Soc. for Neurosci., 20: 631.14, 1994.

103. Kang, C.H., Raszkiewicz, J.L., Turek, J.W., Brioni, J.D., Decker, M.W., Arneric, S.P., and

Sullivan, J.P. Transdermal ABT-418: Pharmacokinetic and pharmacodynamic properties of a cholinergic channel activator (ChCA). Soc. for Neurosci., 20: 631.15, 1994.

104. Briggs, C.A., Hughes, M.L., Monteggia, L.M., Giordano, T., Donnelly-Roberts, D.L., and Arneric,

S.P., Nicotinic acetylcholine receptor electrophysiology and pharmacology of ABT-418 in PC12 cells. Soc. for Neurosci., 20: , 1994.

105. Arneric, S.P., W.J. Jackson, A.V. Terry, Jr., Marsh, K.C., Decker, M.W., Buccafusco, J.J.,

Improvement in performance of a delayed response task by monkeys given ABT-418, a nAChR activator for memory enhancement. Soc. for Neurosci., 20: , 1994.

106. Lin, N.H., He, Y., Anderson, D.J., Garvey, D.S., Wasicak, J.T., Sullivan J.P. and Arneric S.P.

Synthesis and receptor binding properties of novel cholinergic channel ligands as potential cognition enhancers. Soc. for Neurosci., 20: 123.11, 1994.

107. Donnelly-Roberts, D., Arneric, S.P. and Sullivan, J.P. Beta-Amyloid peptides can modulate the

functional activation of human nicotinic acetylcholine receptors. Soc. for Neurosci., 20: 725.1, 1994.

108. Sullivan, J.P., Anderson, D.J., Donnelly-Roberts, D., Garvey, D.S., Williams, M. and Arneric, S.P.

ABT-418: In vitro properties of a novel cholinergic channel activator (ChCA) for the potential treatment of Alzheimer's disease. International Symposium on Nicotine: The Effects of Nicotine on Biological Systems II, Montreal, Canada, July 21-24, 1994.

109. Sullivan, J.P., Anderson, D.J., Pauly, J.R., Williams, M., and Arneric, S.P., [3H]ABT-418: Receptor binding properties of a novel cholinergic channel ligand. International Symposium on Nicotine: The Effects of Nicotine on Biological Systems II, Montreal, Canada, July 21-24, 1994.

110. Sullivan, J.P., Bannon, A.W., Donnelly-Roberts, D., Anderson, D.J., Piattoni-Kaplan, M.,

Gopalkrishnan, M., Decker, M.W., and Arneric, S.P. (±)Epibatidine elicits a diversity of nicotinic receptor-mediated effects. International Symposium on Nicotine: The Effects of Nicotine on Biological Systems II, Montreal, Canada, July 21-24, 1994.

111. Arneric, S.P., Sullivan, J.P. and Williams, M. Cholinergic channel activators (ChCAs) for the

potential treatment of CNS disorders. International Symposium on Nicotine: The Effects of Nicotine on Biological Systems II, Montreal, Canada, July 21-24, 1994.

112. Decker, M.W., Brioni, J.D., Buckley, M.J., Curzon, P., O'Neill, A.B., Kim, D.J.B., Majchrzak, M.J., Kang, C.H., Raszkiewicz, J.L., Turek, J.W., Marsh, K., Quigley, S., Radek, R., Sullivan, J.P., and Arneric, S.P. ABT-418: In vivo profile of a novel cholinergic channel activator (ChCA) for the potential treatment of Alzheimer's disease (AD) International Symposium on Nicotine: The Effects of Nicotine on Biological Systems II, Montreal, Canada, July 21-24, 1994.

113. Piattoni-Kaplan, M., Donnelly-Roberts, D., Pauly, J.R., Hill, W.D., Pan, J.B., Arneric, S.P., and

Sullivan, J.P., Immunocharacterization of the human 7 neuronal nicotinic acetylcholine receptor subunit, International Symposium on Nicotine: The Effects of Nicotine on Biological Systems II, Montreal, Canada, July 21-24, 1994.

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114. Holladay, M.W., Wasicak, J.T., Donnelly-Roberts, D., Anderson, D.J., Pavlik, P., Martin,Y., Sullivan, J.P., and Arneric, S.P., Interaction of ABT-418, nicotine, and their nor- and epi- analogs with cholinergic channel receptors: binding, functional activity, and molecular modeling studies. International Symposium on Nicotine: The Effects of Nicotine on Biological Systems II, Montreal, Canada, July 21-24, 1994.

115. Donnelly-Roberts, D.L., Gopalakrishnan, M., Arneric, S.P., and Sullivan, J.P., Modulation of

human neuronal nicotinic acetylcholine receptor (nAChR) activation by L-type calcium channel antagonists. International Symposium on Nicotine: The Effects of Nicotine on Biological Systems II, Montreal, Canada, July 21-24, 1994.

116. Pauly, J.R., Arneric, S.P., Williams, M. and Sullivan, J.P., Autoradiographic comparison of [3H]-

cytisine and [3H]ABT-418 binding in rat brain. International Symposium on Nicotine: The Effects of Nicotine on Biological Systems II, Montreal, Canada, July 21-24, 1994.

117. Buccafusco, J.J., Jackson, W.J., Terry, A.V., Jr., Marsh, K.C., Decker, M.W., and Arneric, S.P.,

Improvement in performance of a delayed matching-to-sample task by monkeys by ABT-418, a novel nAChR activator from memory enhancement. International Symposium on Nicotine: The Effects of Nicotine on Biological Systems II, Montreal, Canada, July 21-24, 1994.

118. Arneric, S.P., Cholinergic channel activators (ChCAs) for the treatment of Alzheimer's disease.

IBC Conference: Alzheimer's Disease-Advances in Understanding and Treatment, Philadelphia, PA., September 22-23, 1994.

119. Briggs, C.A., Hughes, M.L., Monteggia, L.M., Giordano, T., Donnelly-Roberts, D.L., and Arneric,

S.P., Functional pharmacology of the novel nAChR activator ABT-418 in PC12 cells. The Cholinergic Synapse: Structure, Function and Regulation, Baltimore, Maryland, Nov. 6-10, 1994.

120. Arneric, S.P., Sullivan, J.P., Decker, M.W., Brioni, J.D., Buccafusco, J.J., Briggs, C.A., Marsh,

K.C., Rodrigues, A.D., Donnelly-Roberts, D.L., Pauly, J.R., and Williams, M. Cholinergic channel activators (ChCAs) for the potential treatment of Alzheimer's disease (AD), The Cholinergic Synapse: Structure, Function and Regulation, Baltimore, Maryland, Nov. 6-10, 1994.

121. Gopalakrishnan, M., Bertrand, D., Touma, E., Giordano, A., Campbell, J. Hu, I.C., Buisson, B.,

Donnelly-Roberts, D., Arneric, S.P., and Sullivan, J.P., Stable expression, radioligand binding

and functional properties of the human neuronal nicotinic acetylcholine receptor subtype. FASEB, 9: S2261, 1995.

122. Sullivan, J.P., Monteggia, L.M., Anderson, D., Giordano, A., Arneric, S.P., and Gopalakrishnan

(SPON: M. Williams), Stable expression and pharmacological properties of the human neuronal

nicotinic acetylcholine receptor subtype. FASEB, 9: S2262, 1995. 123. Pendergast, M.A., Buccafusco, J.J., Jackson, W.J., Terry, A.V., Decker, M.W., and Arneric, S.P.

Improvement in performance of a delayed response task by aged monkeys given ABT-418, a novel nAChR activator for memory enhancement. FASEB, Atlanta, April, 1995.

124. Sullivan, J.P., Donnelly-Roberts, D., Briggs, C.A., Holladay, M.W., Decker, M.W., Brioni, J.D.,

Bannon, A.W., Williams, M., and Arneric, S.P., Development of novel cholinergic channel activators (ChCAs): A new therapeutic approach for the treatment of CNS disorders. Western Pharmacology Society, Honolulu, Hawaii, January 22-27, 1995.

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125. Arneric, S.P., Donnelly-Roberts, Hu, I., Decker, M.W., Marsh, K.C., Buccafusco, J.J., and Sullivan, Cytoprotective and cognitive enhancement actions of ABT-418 in primates, XVIIth Int. Symposium on Cerebral Blood Flow and Metabolism, Cologne, Germany, July 2-6, 1995.

126. Elliott, R.L., Kopecka, H., Gunn, D.E., Lin, N.H., Garvey, D.S., Ryther, K.B., Holladay, M.W.,

Anderson, D.J., Campbell, J.E., Donnelly-Roberts, D., Piattoni-Kaplan, M., Sullivan, J.P. and Arneric, S.P., 2-(Aryloxymethyl) azacyclic analogues as novel nicotinic acetylcholine receptor (nAChR) ligands. American Chemical Soc., Chicago IL, August 1995.

127. Arneric, S.P., Bannon, A., Brioni, J.D., Briggs, C.A., Decker, M.W., Elliott, R., Gopalakrishnan,

M., Holladay, M.W., Lebold, S.A., Lin, N.H., Donnelly-Roberts, D., Sullivan, J.P., and Williams. Neuronal nicotinic acetylcholine receptor (nAChR) diversity and therapeutic potential of selective ligands. American Chemical Soc., Chicago IL, August 1995.

128. Holladay, M.W., Daanen, J.F., Wasicak, J.T., Bai, H., Lebold, S.A., Pavlik, P.A., He, Y., Lin, N.H.,

Abreo, M.A., Garvey, D.S., Martin, Y.C., Anderson, D.J., Campbell, J.E., Donnelly-Roberts, D., Piattoni-Kaplan, M., Sullivan, J.P., Williams, M. and Arneric, S.P., Structure-activity and molecular modeling studies on nicotinic acetylcholine receptor (nAChR) ligands. American Chemical Soc., Chicago IL, August 1995.

129. Arneric, S.P., Sullivan, J.P., and Williams, M. Molecular diversity of nAChRs: Opportunities for

the development of cholinergic channel modulators for treatment of CNS disorders. International Symposium on Neuronal Receptor Mechanisms, Niigata, Japan, June 28-29., 1995.

130. Arneric, S.P., Donnelly-Roberts, D., Briggs, C.A., Anderson, D.J., Piattoni-Kaplan, M., Campbell,

J.E., McKenna, D., Hettinger, A.M., Garvey, D.S., Williams, M. and Sullivan, J.P., A-85380: In vitro pharmacological properties of a novel, 40 pM affinity cholinergic channel activator. Soc. for Neurosci., 21: 247.7, 1995.

131. Sullivan, J.P., Gopalakrishnan, M., Monteggia, L.M., Anderson, D.J., Bertrand, D., and Arneric,

S.P., Pharmacological properties of the human nicotinic acetylcholine receptor (nAChR) stably expressed in a mammalian cell line. Soc. for Neurosci., 21: 36.6 , 1995.

132. McKenna, D., Arneric, S.P., and Briggs, C.A., Inhibition of the human nicotinic receptor by MK-801 (Dizocilpine). Soc. for Neurosci., 21: , 1995.

133. Monteggia, L.M., Arneric, S.P., and Sullivan, J.P., RT-PCR analysis of the distribution of

neuronal nicotinic acetylcholine receptors in human peripheral tissue. Soc. for Neurosci., 21: 143.11, 1995.

134. Donnelly-Roberts, D., Anderson, D.J., Gopalakrishnan, M., Campbell, J.E., Piattoni-Kaplan, M.,

Arneric, S.P. and Sullivan, J.P., Continuous infusion of (-)-nicotine differentially affects radioligand binding, cation efflux, and neurotransmitter release. Soc. for Neurosci., 21: 143.7, 1995.

135. Hu, I., Donnelly-Roberts, D., Arneric, S.P., and Sullivan, J.P., In vitro cytoprotective properties of

the novel cholinergic channel activator (ChCA), ABT-418. Soc. for Neurosci., 21: 247.15, 1995. 136. Gopalakrishnan, M., Buisson, B., Touma, E., Giordano, T., Campbell, J.E., Hu, I.C., Donnelly-

Roberts, D., Arneric, S.P., Bertrand, D., and Sullivan, J.P., Stable expression and

pharmacologic properties of the human nicotinic acetylcholine receptor (nAChR). Soc. for Neurosci., 21: 36.8, 1995.

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137. Anderson, D.J., Campbell, J.E., Raszkiewicz, J.L., Hettinger, A.M., Garvey, D.S., Arneric, S.P.,

and Sullivan, J.P., Binding properties of [3H]A-85380, a high-affinity, neuronal nicotinic acetylcholine receptor radioligand. Soc. for Neurosci., 21: 247.8 , 1995.

138. Lin, N.H., Abreo, M.A., Gunn, D.E., Garvey, D.S., Hettinger, A.M., Elliott, R.L., Lebold, S.A.,

Holladay, M.W., Anderson, D.J., Donnelly-Roberts, D., Sullivan, J.P., Arneric, S.P., and William, M. 3-Pyridyl ethers as novel high affinity neuronal nicotinic acetylcholine receptor (nAChR) ligands. Soc. for Neurosci., 21: 247.3, 1995.

139. Arneric, S.P., Bannon, A.W., Briggs, C.A., Brioni, J.D., Decker, M.W., Gopalakrishnan, M.,

Holladay, M.W., Kyncl, J., Lin, Nan-Horng Lin, Marsh, K.C., Qiu, Y., Donnelly-Roberts, D., Sullivan, J.P., and Williams, M., ABT-089: An orally active cholinergic channel modulator (ChCM) with cognition enhancing and neuroprotective properties. American College Neuropsychopharmcology, San Juan, Puerto Rico, Dec. 1995.

140. Wang, Z. Jorge, A, Marsh, K.C., Arneric, S.P., and Wilber D., Effects of nicotinic acetylcholine

receptor agonists on canine atrial electrophysiology. North American Soc. of Pacing and Electrophysiology, May 1996.

141. Arneric, S.P., Bannon, A.W., Briggs, C.A, Brioni, J.D., Buccafusco, J.J., Decker, M.W.,

Gopalakrishnan, M., Holladay, M.W., Kyncl, J., Lin, N.H., Marsh, K.G., Qiu, Y.H., Radek, R., Donnelly-Roberts, D.L., Sullivan, J.P. and Williams, M. ABT-089: an orally active cholinergic channel modulator (ChCM) with cognition enhancing and neuroprotective activity Fourth Interational NIce/Springfield Symposium on Advances in Alzheimer's Therapy. Nice France, April 10-14, 1996.

142. Sullivan, J.P., Xue, I., Bhaste, K., Arneric, S.P. and Donnelly-Roberts, D.L., In vitro

neuroprotective properties of the novel cholinergic channel activator ABT-418 and the acetylcholinesterase inhibitor tacrine. Fourth Interational NIce/Springfield Symposium on Advances in Alzheimer's Therapy. Nice France, April 10-14, 1996.

143. Flood, K., Marsh, K.C., Krill, S.L., Travedi, J. and Arneric, S.P. Sustained-Release Matrix

Systems for a Highly Water-Soluble Compound, ABT-089. AAPS Annual Meeting, Seattle, WA, Oct. 27-31, 1996.

144. Wevers, A., Monteggia, L.M., Maelicke, A., Giacobini, E., Sullivan, J.P., Arneric, S.P., and

Schroder, H. Morbus Alzheimer: Cortical colocalization pattern of nicotinic receptors and pathological markers. Soc. for Neurosci., 22: 87.6, 1996.

145. Anderson, D.J., Donnelly-Roberts, D., Campbell, J., Pauley, P. Magill, Arneric, S.P., and

Sullivan, J.P. Differential effects of ABT-089 and (-)-nicotine on nicotinic acetylcholine receptor density and function following subacute administration. Soc. for Neurosci., 22:502.11, 1996.

146. Campbell, J.E., Sullivan, J.P., Arnold, W., He, Y., Holladay, M.W., Lin, N.H., Daanen, J., Li, Y.,

Marsh, K.C., Peterson, B., Nellans, H., Trivedi, J., and Arneric, S.P. Pharmacokinetic and safety studies on ABT-089; an orally active cholinergic channel modulator. Soc. for Neurosci., 22:502.13, 1996.

147. Decker, M.W., Bannon, A.W., Curzon, P., Gunther, K.L., Brioni, J.D., Holladay, M.W., Lin, N-H.,

Li, Y., Daanen, J., Buccafusco, J.J., Prendergast, M.A., Jackson, W.J., and Arneric, S.P. Effects of ABT-089, a novel cholinergic channel modulator, on cognitive performance in rats and monkeys. Soc. for Neurosci., 22:502.10, 1996.

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148. Donnelly-Roberts, D., Xue, I., Delbono, O., Arneric, S.P., and Sullivan, J.P. The cholinergic

channel activator (ChCA) ABT-418 protectors against gp120 and A(1-42)-induced neurotoxicity. Soc. for Neurosci., 22:749.6, 1996.

149. Kim, D.J.B., Brodie, M.S., Decker, M.W., Arneric, S.P., and Brioni, J.D. ABT-089: Discriminative

stimulus properties and electrophysiological actions. Soc. for Neurosci., 22: 502.9, 1996. 150. Manelli, A., Donnelly-Roberts, D., Arneric, S.P., and Puttfarcken, P.S. Characterization of F11

cells, a dorsal root ganglion cell line: evidence for functional neuronal nicotinic receptors. Soc. for Neurosci., 22:503.26, 1996.

151. Gopalakrishnan, M., Delbono, O., Molinari, E.J., Renganathan, M., Messi, L., Arneric, S.P. and

Sullivan, J.P. Regulation of recombinant human 7 nicotinic receptors by activator and antagonist ligands. Soc. for Neurosci., 22: 603.18, 1996.

152. Sullivan, J.P., Anderson, D.J., Briggs, C.A., Campbell, J.E., Donnelly-Roberts, D.,

Gopalakrishnan, M., Gunn, D., He, Y., Holladay, M.W., McKenna, D., Lin, N.H., Molinari, E., Piattoni-Kaplan, M., Xue, I., Williams, M., and Arneric, S.P. ABT-089: A potent and selective cholinergic channel modulator with neuroprotective properties. Soc. for Neurosci., 22:502.12, 1996.

153. Puttfarcken, P.S., Manelli, A.M., Donnelly-Roberts, D., and Arneric, S.P. ABT-594 and (±)-

epibatidine inhibit capsaicin-evoked substance P (SP) and calcitonin gene related peptide (CGRP) release from rat spinal cord slices via neuronal nicotinic acetylcholine receptors (nAChRs). Soc. for Neurosci., New Orleans, LA, Oct. 1997.

154. Donnelly-Roberts, D., Puttfarcken, P., Jacobs, I.X., Kuntzweiler, T., and Arneric, S.P. ABT-594:

Neuroprotective effects in spinal cord (sc) cultures by a broad spectrum analgesic acting via nicotinic acetylcholine receptors (nAChRs). Soc. for Neurosci.., New Orleans, LA, Oct. 1997

155. Nikkel, A.L., Bitner, R.S., Bannon, A.W., Arneric, S.P. and Decker, M.W. Supraspinal C-fos

induction produced by a novel cholinergic channel modulator analgesic, ABT-594. Soc. for Neurosci., New Orleans, LA, Oct. 1997.

156. Holladay, M.W., Wasicak, J.T., Lin, N.-H., He, Y., Ryther, K.B., Bannon, A.W., Buckley, M.J., Kim,

D.J.B., Decker, M.W., Anderson, D.J., Campbell, J.E., Donnelly-Roberts, D.L., Briggs, C.A., McKenna, D.G., Niforatos, W.E., Piattoni-Kaplan, M., Williams, M., and Arneric, S.P. Identification, initial pharmacological evaluation, and structure-activity relationships of ABT-594 as a potent, orally active analgesic agent acting via neuronal nicotinic acetylcholine receptors. Soc. for Neurosci., New Orleans, LA, Oct. 1997.

157. Decker, M.W., Bannon, A.W., Buckley, M.J., Kim, D.J.B., Holladay, M.W., Ryther, K.B., Lin, N.-H.,

Wasicak, J.T., Williams, M., and Arneric, S.P. Antinociceptive effects of the novel cholinergic channel modulator, ABT-594, in mice. Soc. for Neurosci., New Orleans, LA, Oct. 1997.

158. Bannon. A.W., Decker, M.W., Curzon, P., Buckley, M., Kim, D., Lynch, J.K., Wasicak, J.T.,

Arnold, W.H., Holladay, M.W., Arneric, S.P. Characterization of ABT-594 in rats: a novel, orally effective antinociceptive agent acting via nicotinic acetylcholine receptors. Soc. for Neurosci. , New Orleans, LA, Oct. 1997.

159. Kim, D.J., Bannon, A.W., Campbell, J.E., Lynch, J.K., Bai, H., Holladay, M.W., Arneric, S.P. and

Decker, M.W. Efficacy of ABT-594, a novel antinociceptive agent acting via nicotinic acetylcholine receptors in a model of neuropathic pain. Soc. for Neurosci., New Orleans, LA, Oct. 1997.

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160. Arneric, S.P., Anderson, D.J., Campbell, J.E., Kuntzweiler, T., Wasicak, J., Holladay, M.W., Pauly, J., Williams, M., and Donnelly-Roberts, D. In vitro pharmacology of ABT-594: a novel, non-opioid analgesic, neuronal nicotinic acetylcholine receptor (nAChR) ligand. Soc. for Neurosci., New Orleans, LA, Oct. 1997.

161. Jacobson, P.B., Komater, B., Wilcox, D.M., Namovic, M.T., Harris, R.R., Decker, M.W., Holladay,

M.W., Arneric, S.P., Anti-inflammatory Activity of ABT-594 [R(R)-5-(2-Azetidinylmethoxy)-2-Chloropyridine]: A Novel, Non-Opioid Nicotinic Acetylcholine Receptor Agonist. American Society for Experimental Therapeutics, San Franscico, April, 1998.

162. Schroder, H., Wevers, A., Nowacki, S., Giacobini, G., deVos, R., van Noort, G., Schutz, U., Liu,

W., Monteggia, L., Arneric, S.P., Lindtrom, J., Moser, N., Witter, B., Maelicke, A., Nicotinic receptors in Alzheimer's disease (AD) and aging. Fourth Interational Nice/Springfield Symposium on Advances in Alzheimer's Therapy. Geneva, Switzerland, April , 1998.

163. Li, Y., Lin, N-H., Wagenaar, F., Lee, E., Anderson, D.J., Kuntzweiler, T., Arneric, S.P., and

Holladay, M.W., Synthesis and structure-activitity relationships of the 6-chloro-5-substituted analogs of the 3-[2-((S)-pyrrolidinyl)-methoxy]pyridine, A-84543, a potent nicotinic acetylcholine receptor agonist. American Chemical Soc., Boston, August, 1998.

164. Dussor, G.O., Leong, A.S, Gracia, N.B., Hargreaves, K.M., Arneric, S.P., and Flores, C.M.,

Differential effects of neuronal nicotinic receptor agonists on capsaicin-evoked CGRP release from peripheral terminals of primary sensory neurons. Soc. for Neurosci., Los Angeles, CA, Oct. 1998.

165. Anderson, D.J., Campbell, J.E., Lee, E., Holladay, M.W., Surber, B., Thomas, S., Arneric, S.P.,

Kuntzweiler, T.A., [3H]ABT-594 is a high-affinity, selective neuronal nicotinic acetylcholine receptor ligand. Soc. for Neurosci., Los Angeles, CA, Oct. 1998.

166. Arneric, S.P., Bannon, A.W., Decker, M.W., Holladay, M.W., Curzon, P., Donnelly-Roberts, D.,

Puttfarken, P.S., Bitner, R.S., Diaz, A., Dickenson, A.H., Porsolt, R.D., Williams, M. Selective Modulation of neuronal nicotinic acetylcholine receptors: A novel approach to provide broad spectrum pain relief. American College of Neuropsychopharmacology, Puerto Rico, Dec., 1998.

167. McElroy, J., Wiedemann, K.A., Zeller, K.L., Jones, K.W., Arneric, S.P., Acute efficacy of the

substance P antagonist L-733,060 in rat learned helplessness, a chronic animal model of depression. Soc. for Neurosci., Miami, FLA, Oct. 1999.

168. Wilde, R.E., Klaczkiewicz, J.D., Carter, K.L., Gilligan, P.J., Olson, R.E., Frietze, W.E., Buckner,

W.H., Beck, J.P., Curry, M.A., Robertson, D.W., Sun, J.H., Arneric, S.P., Hartig, P.R., Fitzgerald, L.W., Marshall, W.J., Retro-Purines: Nonpeptide Corticotropin-Releasing Factor Receptor Ligands. 219th ACS National Meeting, San Francisco, CA, March 26-30, 2000, p.317.

169. Wilde, R.G., Crter, K.L., Klaczkiewicz, J.D., Gilligan, P.J., Olson, R.E., Frietze, W.E., Buckner, W.H., Beck, J.P., Curry, M.A., Arvanitis, A.G., Mical, A.J., Robertson, D.W., Trainor, G.L., Fitzgerald, L.W., McElroy, J.F., and Arneric, S.P., Retro-purine CRF antagonists: SAR refinement of the aryl and side-chain groups. 220th ACS National Meeting, Washinton D.C., August 20-24, 2000, #123.

170. Gilligan, P.J., He, L., Clarke, T., Fitzgerald, L.W., McElroy, J., Grossman, S., Arneric, S. Tivitmanhaisoon P., Pyrazolo-[1,5-a]-1,3,5-triazine CRF receptor antagonists: Synthesis and structure-activity relationships of 8-(substituted phenyl) analogs. 220th ACS National Meeting, Washinton D.C., August 20-24, 2000, #125.

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171. He, L., Gilligan, P.J., Clarke, T., Fitzgerald, McElroy, J., Grossman, S., Arneric, S. Pyrazolo[1,5-a]-1,3,5-triazine CRF receptor antagonists: Synthesis and structure-activity relationships of 8-heteroaryl analogs. 220th ACS National Meeting, Washinton D.C., August 20-24, 2000, #126.

172. Arvanitis, A.G., Rescinito, J.T., Arnold III, C.R., Wilde, R.G., Gilligan, P.J., Olson, R.E., Frietze, W.E., Robertson, D.W., Sun, J.H., Yan J-S, Christos, T.E., Cain, G.A., Teleha, C.A., Hartig, P.R., Fitzgerald, L.W., McElroy, J., Grossman, S., Zaczek, R., Arneric, S.P., Imidazo[4,5-b] and imidazo[4,5-c]pyridines as corticotropin releasing factor ligands. 220th ACS National Meeting, Washinton D.C., August 20-24, 2000, #156.

173. Buccafusco, J.J., Terry, A.V., Predergast, M.A., Smith, M.A., and Arneric, S.P., Cognitive aspects of potential drugs of abuse in macaques. Soc. for Neurosci., New Orleans, LA, 30th Annual Meeting, Nov., 2000, 753.19.

174. Ho, S.P., Takahashi, L.K., Livanov, V., Spencer, K., Lesher, T., Maciag, Smith, M.A., Hartig, P.A., and Arneric, S.P., Anxiolytic effects induced by antisense inhibition of brain corticotrophin releasing factor-2 receptors. Soc. for Neurosci., New Orleans, LA, 30th Annual Meeting, Nov., 2000, 851.5.

175. Takahashi, L.K., Ho, S.P., Livanov, V., and Arneric, S.P., Antagonism of CRF2 receptors produces anxiolytic effects in models of anxiety. Soc. for Neurosci., New Orleans, LA, 30th Annual Meeting, Nov., 2000, 851.6

176. Lelkes, Z., Arneric, S.P., Hajos, M. Effects of [S,S]-Reboxetine, a selective inhibitor of

noradrenaline reuptake, on sleep in rats. 17th ESRS Congress on European Sleep Research Soc. Oct 6-9, 2004, Prague.

177. Jiang, X., Dong, H., Lam, J.K., Giesz, S., Janke, D., Khawaja, A, Mezeyova, J., Parker, D.B.,

Arneric, S.P., Snutch, T.P., Belardetti, F., Ambroxol Block of Voltage-Gated Ca2+ Channels, Soc. for Neurosci., Atlanta 36th Annual Meeting, Nov., 2006.

178. Wyche, A., Xu, S., Kim, D., Simonson, E., Pajouhesh, H., Arneric, S.P., Snutch, T.P., and

Parker, D.,Factors Affecting In Vitro Microsomal Metabolic Stability Assays, SBS, Toronto, April, 2007.

179. Lam, J., Jiang, X., Hendricson, A., Tringham, E., Belardetti, F., Arneric, S.P., Snutch, T.P., and Parker, D.B., Rat Cav2.1 stable cell line expression in HEK 293 cells.SBS, Toronto, April, 2007.

180. Mezeyova, J., Jiang, X., Khawaja, A. Larsen, A, Lam, J.K., Tringham, E. Belardetti, F., Snutch,

T.P., Arneric, S.P., Parker, D.B., Optimization of recombinant Cav2.2 cell lines in HEK293 cells, Soc. For Neurosci., San Diego 37th Annual Meeting, Nov. 2007.

181. Hajos, M., Krause, M., Hoffman, W.E., Hajos-Korcsok, E., Yu, J.H., Robinson, D.D., Wall, T.M.,

Higdon, N.R., Svensson, K.A., Nichols, N.F., Rodney, W., Groppi, V.E., Arneric, S.P., Hurst, R.S. Efficacy of a novel α7 nicotinic acetylcholine receptor agonist after acute and repeated administration, and after chronic nicotine exposure , Soc. For Neurosci., San Diego 37th Annual Meeting, Nov. 2007.

182. Gallen, C.G., Parker, D.B., Tringham, E.W., Pajouhesh, P., Janke, D., Belardetti, F., Arneric,

S.P., and Snutch, T.P., Development of a cell-based screening assay and identification of a novel class of T-type calcium channel blocker. ASENT, Washington, D.C., 2008.

183. Snutch, T.P., Garcia, E., Tyson, J., Parker, D.B., Tringham, E.W., Pajouhesh, H., Belardetti, F.,

Arneric, S.P., Development of cell-based screening assay and identification of novel T-type calcium channel blockers. Calcium Channel Meeting, Kiev, June 2008.

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184. Stinnette, W.T., Ruble, C.L.A, Arneric, S.P., 6TM and 7-TM variants of the -opioid receptor (MOR) in human and mouse tissues. Soc. For Neurosci., San Diego, Nov. 2013.

185. Arneric, S.P., Strategies for new target development of pain therapeutics, SIMPAR-2014, Rome, Italy, March 28, 2014.

186. Rankovic, Z., Bures, M.G., Wang, X-S., Heinz, B., Burris, K., Alberts, J.J., Kennedy, J.D., Li, D., Hahn, P.J., Gernert, D.L., Stevens, F.C., Arneric, S.P., Structure–Functional Selectivity Relationship Studies of Novel G-protein Biased Mu Opioid Receptor (B-MOR) Agonists, Chemistry Gordon Conference, 2014.

187. Arneric, S.P., Zhang, J., Miller, P.E., Rankovic, Z., Hahn, P.J., Gernert, D.L., Ghetti, A., Action of Biased–MOR Agonists to Inhibit Depolarization-Induced Calcium Mobilization in Cultured Human DRG Neurons. International Assciation for the Study of Pain (IASP- Buenes Aires, Argentina, Oct 2014).

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