Agonist-receptor efficacy. I: Mechanisms of efficacy and receptor promiscuity.
The description of drug effects on receptor proteins is based on models and equations used to describe mass-action kinetics of molecules and inert surfaces. These models provide an adequate description of drug affinity, that is, how well a molecule binds to a receptor protein, but the way in which ligands change receptor populations to impart signals to cells remains to be determined. In the first of two articles, Terry Kenakin discusses a basic question in receptor pharmacology, namely the nature of ligand efficacy.
Kenakin
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Department of Cellular Biochemistry, Glaxo Research Institute, Research Triangle Park, NC 27709, USA.
D000818:Animals; D006801:Humans; D011955:Receptors, Drug / Q000819:agonists* / Q000737:chemistry
D011955:Receptors, Drug