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-ligand binds weakly (ionic) -receptor changes shape -ligand binds more tightly -receptor activates |
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| -ability of a bound drug to change a receptor in a way that produces an effect |
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| drug that occupies and activates a receptor producing a cellular response |
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| -drug that occupies a receptor and prevents agonist from binding |
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-receptor antagonists -physiological antagonists -chemical antagonists |
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| -drug binds but does not activate |
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-drug binds to a DIFFERENT receptor -produces an opposite effect |
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| -interacts directly with the drug |
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-Clark -effect is proportional to number of receptors occupied |
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| modified occupation theory |
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-Ariens -100% occupancy does NOT equal max response -intrinsic effect determines effect produced by drug (0 to 1) |
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-effect is determined by rate dissociation -high dissociation equals high potency |
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-only R* can produce response -agonists increase R* -inverse agonists preferably bind to R so decrease R* |
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