Chap 5 ppts - Receptor terminology Protein-ligand...

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1 Receptor terminology Protein-ligand properties: specificity, saturation, affinity, competition Antagonist: binds to receptor site and inhibits Agonist: binds to receptor site and stimulates Down-regulation: levels of messenger →↓ receptors Up-regulation: levels of messenger →↑ receptors Supersensitivity: cell response to up regulation
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2 Receptor types A. Intracellular receptors (steroid, thyroid hormones) B. Cell membrane receptors i. ion selective channels (acetyl choline) ii. receptor has enzyme activity (insulin) iii. receptors acting via G proteins a. adenylate cyclase ( β adrenergic, glucagon, TSH, etc.) b. phospholipase C ( α adrenergic, angiotensin II, etc.) (b. G proteins directly on ion selective channels-ignore)
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3 A. Intracellular receptors Examples: thyroid hormones (T 3 4 ), steroids (estrogen, progesterone, testosterone, aldosterone, cortisol) fig 5-4
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4 B i. Ion selective channels e.g. acetyl choline (nicotinic), many CNS neurotransmitters (glutamate, glycine, GABA) fig 5-5a
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5 B ii. Receptor has enzyme activity fig 5-5b
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This note was uploaded on 03/26/2012 for the course PHSL 310 taught by Professor Ferraro during the Fall '11 term at SIU Carbondale.

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Chap 5 ppts - Receptor terminology Protein-ligand...

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