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Systems Pharmacology
Effects of Drug Receptor Binding
14
Biology
Graduate
11/13/2011

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Cards

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