PCL302H1 Lecture 3: Lecture 3 - Receptor Quantitation II.pdf
28 Sep 2014
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Objectives: agonists (potency and efficacy, deviations from predicted dose-response relationships, threshold effects, spare receptor effects, antagonists & inverse agonists, drug selectivity . Receptor activity: receptors have different conformations , basal situation: Little or no effect: an agonist stabilizes the active conformation: Efficacy of an agonist: the amount of an effect, or change in physiology, that an agonist can produce. By an agonist only: efficacy depends on ability of the agonist to stabilize an active state of the receptor. Response: as drug concentration increases so does physiological response d n u o b m p d e s n o p s e. When ec50= kd response a drug can produce. Typically sigmoidal: at some point adding more agonist does not produce more effect, this is emax. Same amount of maximal activity as the endogenous compound. Shows less of the response compare to endogenous compound. Full agonists: strong physiological effect that mimics the action of an endogenous ligand.
