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11 Cards in this Set
- Front
- Back
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What does an agonist do?
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Stimulates receptor
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What does an antagonist do?
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Blocks response to agonist, binds to receptor, doesn't initiate response
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What does a partial agonist do?
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Can't produce the same Emax response, can act as a competitive inhibitor in presence of full agonist, binds to receptor, displaces agonist and dec agonist effect
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What does affinity mean?
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Measure of binding of drug to receptor
Kd = concentration needed to produce half maximal binding |
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What does potency mean?
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Dose required to produce given effect
EC50 - dose required for half-maximal effect |
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What does efficacy mean?
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Degree of biological response produced by the drug
Intrinsic response, ability to initiate response |
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What is a competitive antagonist?
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Will displace agonist, incapable of activating mechanism
Dec Affinity, Inc EC50, no effect on max response |
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What is a Noncompetitive antagonist?
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Irreversibly binds to same site as agonist or binds to secondary site which influences active site
Dec Emax, no change of Kd or EC50 |
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What is a functional/physiological antagonist?
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Acts through a completely different mechanism than the agonist to counter the agonist's effects
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What is a chemical antagonist?
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Antagonist which interacts directly w/agonist and neutralizes it chemically
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What is an inverse agonist?
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Drug that have higher affinity for the inactive state of the receptor, pushing equilibrium to inactive state
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