Term
| how do you calculate Therapeutic Index? |
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Definition
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Term
| in a radioligand binding study, why is the curve a hyperbolic shape? |
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Definition
| Because there is a finite number of receptors |
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Term
| what information can you gain from a dose-responce curve? |
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Definition
Potency (along x-axis)
Slope - large slope is small increase in potency causes large increase in effect
Max efficiacy - y axis
Variability
vertical component: range of effects
horizontal component: range of doses |
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Term
| how does a competitive antagonist effect a dose responce curve? |
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Definition
| Shifts to the right (less potent) but doesn't change max effect of agonist |
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Term
| how does a non-competitive antagonists effect the dose responce curve? |
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Definition
Shifts to the right (less potent) and reduces the mex effect
Bind irreversibly to the receptor |
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Term
| how would spare receptors effect the dose responce curve in the presense of a non-competitive inhibitor? |
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Definition
| a maximal responce to the agonist would still be possible because not all of the receptors are occupied to produce a maximal responce, but once the spare receptors are depleted the max effect would be reduced |
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Term
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Definition
| Potency of drug (smaller ED50 means the drug is more potent) |
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Term
| what is the potency of a drug? |
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Definition
| The dose of a drug needed to produce a max effect (x-axis) |
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Term
| what is the affect of full agonists? |
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Definition
| binds activated receptor to increase drugs responce bc it favors the activated receptor |
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Term
| what's the effect of a partial agonist? |
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Definition
| it favors equilibrium between the active and inactived receptors so it produces less than maximal responce |
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Term
| whats the effect of a inverse agonist? |
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Definition
| it has a higher affinity for the inactive form of the receoptor so in pulls equilibrium towards inactive state |
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Term
| whats the effect of an antagonist? |
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Definition
| it can bind to active or inactive form so no overall effect is produced (horizontal line) |
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Definition
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