351 PHL 5th lecture Effect of Certain Agonist and Their Antagonist on Isolated Guinea Pig Ileum Awatif B. Al-Backer.

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351 PHL 5th lecture Effect of Certain Agonist and Their Antagonist on Isolated Guinea Pig Ileum Awatif B. Al-Backer

It’s the lower part of the small intestine. Involuntry muscle. Guinea Pig Ileum It’s the lower part of the small intestine. Involuntry muscle. Recives sympathetic & parasympathetic innervations. Advantages of GPI: No myogenic contraction More sensitive to histamine Awatif B. Al-Backer

Types of receptors in GPI 1- Cholinergic receptors 2- Serotonergic or tryptaminergic receptors (5-HT1→5-HT7) 3- Histaminergic receptors Awatif B. Al-Backer

Cholinergic receptors 1- Nn R Agonist: Dil. Nicotine Antagonist: Conc. Nicotine 2- M3R Agonist: Ach Antagonist: Atropine Awatif B. Al-Backer

Serotonergic or tryptaminergic receptors Serotonin = 5-HT(5-hydroxytryptamine) 5-HT receptors in GPI: 5-HT2A Agonist: serotonin Antagonist: ketanserin methysergide cyproheptadine (blocks 5-HT2A & H1) Awatif B. Al-Backer

Histaminergic receptors R subtype Distribution Action Agonist Antagonist H1 Smooth muscles contraction Histamine Mepyramine cyproheptadine H2 Gastric mucosa Gastric acid secretion Cimetidine Ranitidine H3 Presynaptic Autoregulation of H release Thioperamide N.B. Histamine acts by stimulating Gs protein → ↑ cAMP → ↑ [Calcium]ic → contraction Awatif B. Al-Backer

e.g. Barium chloride (Bacl2) Direct spasmolytic: e.g. Papaverine Direct acting drugs Direct spasmogen: e.g. Barium chloride (Bacl2) Direct spasmolytic: e.g. Papaverine Awatif B. Al-Backer

Experiment Awatif B. Al-Backer Keys: Hist.=histamine AH= antihistamine N W+N W+N W+N Ach 0.1ml Hist. 0.1ml W+N 0.1ml Bacl2 W+N AH 0.2 ml Hist. 0.1ml Ach 0.1ml 5-HT 0.1ml Atropine 0.1ml Bacl2 0.1ml Papaverine 0.1ml Keys: Hist.=histamine AH= antihistamine 5-HT=serotonin Awatif B. Al-Backer

Experiment Identification of site of action of an unknown drug using isolated guinea-pig ileum N N W+N W+N W+N 0.1 ml 0.1 ml Ach Hist. Unk. 0.1 ml 0.1 ml Unk. 0.2 ml 0.2 ml Unk. Atrop. Ach AH Hist Keys: Ach= acetylcholine Hist.=histamine AH= antihistamine Unk.= unknown Awatif B. Al-Backer