Term
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Definition
-isolated muscle fibers
-2 compounds competing for a 3rd but unknown substrate |
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Term
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Definition
-microbiologist
-1st receptor
-stereoselectivity
-lock and key |
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Term
| binding properties of receptors |
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Definition
-Drug Specificity
-Reversibility
-Stereoselectivity
-Saturability
-Tissue Specificity |
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Term
| failure to satisfy binding properties indicates |
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Definition
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Term
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Definition
| -chemicals that bind to receptors |
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Term
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Definition
-how well a ligand binds a receptor
-NOTHING to do with what effect a ligand has
-Kd measures |
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Term
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Definition
| ability of a bound drug to change receptor in a way that produces an effect |
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Term
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Definition
| -at low concentration a ligand produces an effect |
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Term
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Definition
-concentration of drug where 50% of receptors are complexed with drug
-inversely related to affinity
-directly related to side effects? |
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Term
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Definition
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Term
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Definition
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Term
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Definition
-drug that occupies and activates a receptor, producing a cellular response
-possess both affinity and efficacy |
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Term
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Definition
| drug that occupies a receptor and prevents an agonist or endogenous compound from binding |
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Term
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Definition
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Term
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Definition
| -less than maximal efficacy |
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Term
| 100% occupancy does not equal |
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Definition
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Term
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Definition
-receptor antagonists
-physiological antagonists
-chemical antagonists |
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Term
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Definition
| -binds but does not activate |
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Term
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Definition
-drug that binds to a different receptor
-produces an opposite effect of drug of interest
-has efficacy at a different receptor |
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Term
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Definition
-interacts directly with the drug
-removes it or prevents it from binding
-does not depend on interaction with drug's receptor |
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Term
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Definition
-Clark
-effect produced is proportional to number of receptors occupied |
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Term
| modified occupation theory |
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Definition
-Ariens
-intrinsic activity (alpha) determines effect produced by the drug
-(good agonists=1) |
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Term
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Definition
-Paton
-effect is determined by rate of association/dissociation
-dissociate rapidly=potent |
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Term
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Definition
-receptor exist in a resting and active state
-inverse agonists bind to resting form and decrease number of active receptors |
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