Agonist-receptor efficacy I: mechanisms of efficacy and receptor promiscuity
T Kenakin - Trends in Pharmacological Sciences, 1995 - cell.com
T Kenakin
Trends in Pharmacological Sciences, 1995•cell.comThe 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.
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.
Abstract
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.
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