Lecture-11 Drug Receptors II

Lecture-11 Drug Receptors II - An example of a receptor 3D...

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3D computer rendering of the nicotinic acetylcholine receptor. An example of a receptor
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Scatchard Plot: Regraphing specifically bound drug vs. specifically bound over free drug yields a Scatchard plot.
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Bound Bound/free Higher affinity Drug Lower affinity Drug Interpretation of Scatchard plots On the Scatchard plot, which drug has higher affinity?
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Bound Bound/free High affinity binding site Low affinity binding site B max B Multiple site (or cooperative) binding to a receptor As I stated in class, for the lower affinity This B is
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Different ‘cold’ compounds can compete with the radioligand for binding to the receptor. These compounds will have different affinities for the receptor and thus have different potencies for competing with the radioligand. The order of drug IC 50 values should correlate with their in vivo potencies.
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Drugs compete over a 100-fold concentration range Single sites of receptors become fully occupied over a 100-fold concentration range of drug (two decades on a log scale).
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