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313PHL Lab #4 Identification of effect and site of action of an unknown drug using isolated guinea-pig ileum. Guinea pig ileum is a smooth muscle receive dual nerve supply from autonomic nervous system (sympathetic and parasympathetic) . - PowerPoint PPT Presentation
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313PHLLab #4
Identification of effect and site of action of an unknown drug using isolated guinea-pig ileum
Guinea pig ileum is a smooth muscle receive dual nerve supply from autonomic nervous system (sympathetic and parasympathetic) .
Parasympathetic tone is dominant in ileum which Ach cause contraction by stimulating M3-R .
Why Guinea pig ileum is used?
1. No myogenic contraction so any drug induce contraction can be seen.
2. Very sensitive to histamine unlike the rabbit due to the presence of histaminase enzyme.
Types of receptors present in guinea-pig ileum
Cholinergic receptors .
Serotonergic or tryptaminergic receptors (5-HT1→5-HT7) .
Histaminergic receptors .
Adrenergic receptors .
Types of receptors in guinea-pig ileum:
1- Cholinergic receptors:
Receptor Agonist Antagonist
nicotinic neuronal receptor (Nn- R)
Dil. Nicotine Conc. Nicotine
muscarinic receptor(M3 -R)
Ach Atropine
Types of receptors in guinea-pig ileum:
2-Serotonergic or tryptaminergic (5-HT )receptors :
Serotonin = 5-HT(5-hydroxytryptamine) . 5-HT2A receptor found in smooth muscle and bronchi .
Receptor Agonist Antagonist
5-HT2A serotonin -Methysergide & ketanserin (selective) .
-cyproheptadine (non selective block both H &5-HT receptors) .
Types of receptors in guinea-pig ileum:
3- Histaminergic receptors:
• Histamine is an autacoids naturally occurring in the body .
Receptor distribution Action Agonist Antagonist
H1 Smooth muscles
contraction Histamine Mepyramine
cyproheptadine
H2 Gastric mucosa
Gastric acid secretion
Histamine Cimetidine
Ranitidine
H3 Presynaptic Decrease release of Histamine
Histamine Thioperamide
Types of receptors in guinea-pig ileum:
4- Adrenergic receptors:
Receptor Agonist Antagonist
α1 Adrenaline phentolamine
ß 2Adrenaline -
Types of drugs act on guinea-pig ileum :
Spasmogens:
1- Cholinergic stimulants , e.g. Ach .
MOA :
2- Histaminergic stimulants, e.g. Histamine .
MOA:
histamine act on H1 R which coupled with Gαq → stimulate PLC
→ Hydrolysis of (PIP2) into:
1- DAG → ↑opening of Ca+2 channels
2- IP3 → mobilization of Ca+2 from its stores
1&2 → ↑ intracellular Ca+2
→ Contraction .
Spasmogens:
3- Serotonergic stimulants .
e.g. Serotonin.
4- Direct acting stimulants (spasmogens) .
e.g. Barium chloride, Calcium chloride .
Spasmolytics :
1- Direct acting Spasmolytics .
e.g. Mgcl2
Papaverine
Experiment
Identification of effect and site of action of an unknown drug using isolated guinea-pig ileum
Unknown
Agonist
Blocker+
Agonist+
Unknown