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Metabotropic Receptor: Agonists and AntagonistsMetabotropic receptors act through a second messenger to modulate the actions of excitatory and inhibitoryneurotransmitters. Most metabotropic neuroreceptors are G protein-coupled and have a much longer-lasting effect than ionotropic receptors. Compounds that modulate these neuroreceptors are available from Cayman.

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Glutamate ReceptorsItem No. Product Name Summary

11986 Biphenylindanone AA selective, positive allosteric modulator of mGluR2 (EC

50s = 33.2 and 96 nM in rat and human,

respectively)

11988 Cinnabarinic Acid A partial receptor agonist of mGlu4, effective at 100 µM

16792 Kynurenic Acid Antagonizes glutamate receptor subunit ζ-1 (Ki = 5.4 µM)

14693 LY341495 A selective mGluR2 and mGluR3 antagonist (IC50

s = 21 and 14 nM, respectively)

14961 MTEP (hydrochloride) A negative allosteric modulator of the mGlu5a receptor subtype (Ki = 42 nM; IC

50 = 110 nM)

14411 (S)-3,5-DHPG mGluR1a and mGluR5a agonist (Ki = 0.9 and 3.9 µM, respectively)

Dopamine ReceptorsItem No. Product Name Summary

14598 Bromocriptine (mesylate) Dopamine D2 receptor agonist (K

i = 2.5 nM)

10488 Bupropion (hydrochloride) A Dopamine and norepinephrine reuptake inhibitor (IC50

= 6.5 and 3.4 µM, respectively)

15622 GBR 12909 (hydrochloride) A Dopamine uptake inhibitor (IC50

= 1-51 nM)

16149 L-DOPA methyl ester (hydrochloride) A metabolic precursor of dopamine that crosses the blood-brain barrier

15631 SCH 23390 (hydrochloride) A Dopamine D1-like receptor subtypes D

1 and D

5 antagonist (K

is = 0.2 and 0.3 nM, respectively)

15067 (±)-SKF 81297 (hydrobromide) A selective agonist of the dopamine D1-like receptor (K

i = 1.9 nM)

11984 Sumanirole Maleate Dopamine D2 receptor agonist (K

i = 9 nM)

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For more information on Metabotropic Receptor: Agonists and Antagonists and to view our full line of products, please visit www.CaymanChem.com

Muscarinic Acetylcholine ReceptorsItem No. Product Name Summary

12008 AtropineNon-selective, competitive antagonist of the mAChR types M

1, M

2, M

3, M

4, and M

5 (pKBs range from

8.9-9.8)

16214 Benztropine (mesylate) A centrally acting M1 mAChR antagonist (K

i = 0.59 nM in rat)

15393 BQCAA positive allosteric modulator of the M

1 mAChR that reduces the concentration of acetylcholine

required to activate M1

14574 4-DAMPA potent antagonist of the M

3 mAChR (pK

i = 9.3); also has a high affinity for the M

5 receptor (pK

i =

8.9)

15773 Tiotropium (bromide)A long-acting mAChR antagonist that binds equally to human muscarinic M

1, M

2, and M

3 receptors

(Kds

= 0.04, 0.02, and 0.01 nM, respectively)

15027 Tolterodine (tartrate)A competitive antagonist of mAChRs (K

i = 1.4, 2.7, 3.6, 3.1, and 2.2 nM for M

1 through M

5,

respectively)

16606 Tropicamide An M4 mAChR antagonist (pK

i = 7.2 in chicken heart)

10790 Xanomeline oxalateA potent agonist of mAChRs (EC

50 values are 0.3, 92.5, 5, 52, and 42 nM for M

1, M

2, M

3, M

4, and M

5,

respectively)

Serotonin ReceptorsItem No. Product Name Summary

10011546 AL 34662A 5-HT2 receptor agonist (IC

50s = 0.77 and 1.5 nM in human and rat cerebral cortex homogenates,

respectively-1.5 nM)

12059 Clozapine A partial agonist at the 5-HT1A receptor (pKi = 7)

16752 Palonosetron (hydrochloride ) Selective antagonist of 5-HT3 (pK

i = 10.4 in rat cortex)

10096 SB 242084 (hydrochloride) A 5-HT2C

receptor antagonist (pKi = 9.0)

14692 Tegaserod MaleateA 5-HT

4 agonist (K

i = 3.9-31 nM); also acts as an antagonist for the 5-HT

2A, 5-HT

2B, and 5-HT

2C

receptors (Ki = 32, 3.9, and 100 nM, respectively)

15936 Volinanserin A selective 5-HT2A

antagonist (Ki = 0.36-0.85 nM)

14599 WAY-100635 Maleate A potent, silent antagonist of serotonin 5-HT1A

receptors (IC50

= 2.2 nM; Ki = 0.8 nM)

15871 Zolmitriptan A 5-HT1B

and 5-HT1D

agonist (Kis = 2.2 and 0.92 nM, respectively)