Estimation of agonist affinity and efficacy by direct, operational model-fitting.
A few years ago Black and Leff (1983) presented a theoretical model for agonist action that can be fitted directly to experimental agonist concentration-effect data in order to estimate affinities and relative efficacies of agonists. The model has been successfully applied to data obtained using experimental designs commonly employed in pharmacologic experiments. This article describes the methodology used to fit the model equations to data for full and partial agonists, shows how affinity and efficacy estimates are calculated for these values, and shows how experimental design influences these calculations.
Leff
P
P
Department of Pharmacology, Wellcome Research Laboratories, Beckenham, Kent, United Kingdom.
Prentice
D J
DJ
Giles
H
H
Martin
G R
GR
Wood
J
J
D008954:Models, Biological; D004364:Pharmaceutical Preparations / Q000378:metabolism*; D011955:Receptors, Drug / Q000187:drug effects* / Q000378:metabolism
D004364:Pharmaceutical Preparations; D011955:Receptors, Drug