Lecture-12 Drug Receptors III

Lecture-12 Drug Receptors III - Graphical depictions of...

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Graphical depictions of potency and efficacy A and B are full agonists while C is a partial agonist. Note the dissociation of potency & efficacy: C is more potent than B but B is more efficacious than C.
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Question: If a full agonist and a partial agonist have similar potencies, what would you expect to happen if the two are combined, compared to the effect seen with just the full agonist? At low concentrations , (significantly below K d ) the full agonist and partial agonist would not compete appreciably for binding sites on receptors and thus their effects would be roughly additive. At saturating concentrations they would compete for binding and the effect observed would be somewhere between the effects seen with partial agonist and full agonist applied alone.
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Possible effects of drug on a receptor 1. Occupation theory - drug acts only as long as it occupies the receptor (analogous to a sound being emitted by an organ as long as the key remains pressed). 2. Rate theory - drug action is proportional only to the rate of combination between the drug and the receptor (analogous to pressing a key on a piano where sound is only emitted when the key is first depressed).
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Competitive, irreversible and non- competitive antagonism Competitive antagonists shift agonist concentration-response curves to the right but do not affect the maximal
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This note was uploaded on 02/08/2010 for the course BIO 51310 taught by Professor Sisson during the Spring '08 term at University of Texas at Austin.

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Lecture-12 Drug Receptors III - Graphical depictions of...

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