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Systems Pharmacology
Measuring Effects produced by Agonists/Antagonists
11
Biology
Graduate
11/09/2011

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Term
graded
Definition
response measured on a continuous scale
Term
competitive antagonists shirt the Dr curve
Definition
to the right without affecting maximum response
Term
irreversible antagonist
Definition
effect cannot be overcome by more drug
Term
the move the curve is shifted to the right
Definition
the longer the tissue has been incubated with irreversible antagonist
Term
receptor reserve/spare receptors
Definition
-max effect does NOT require occupation of all receptors by agonist
-low conc. of irreversible antagonists may bind and a max response can still be achieved
-receptor number exceeds the effectors available
-receptor number and effector number can vary between tissues
Term
in the presence of spare receptors
Definition
-Kd is higher than E50
-needs LESS than 50% of receptors occupied to achieve 50% of max response
Term
competitive antagonists
Definition
change in potency, not efficacy
Term
noncompetitive antagonists
Definition
-change in efficacy not potency
Term
noncompetitive antagonist in the presence of spare receptors
Definition
potency and efficacy change
Term
quantal dose response curves
Definition
-response is an either/or event
-related dose and frequency of response in a population of individuals
Term
therapeutic index
Definition
-quantifies the safety margin of a drug in a population of people
-TD50/ED50
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