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Errors in agonist affinity estimation: do they and should they occur in isolated tissue experiments?

作者信息

Leff P, Dougall I G, Harper D H, Dainty I A

机构信息

Department of Pharmacology, Fisons Research and Development Laboratories, Loughborough, UK.

出版信息

Trends Pharmacol Sci. 1990 Feb;11(2):64-7. doi: 10.1016/0165-6147(90)90319-4.

Abstract

Two plausible theories of agonist action - the isomerization and ternary complex mechanisms - predict that agonist affinity measured using the inactivation method may be subject to overestimation. Moreover, the greater the intrinsic efficacy, the greater the predicted error. But are these predictions correct, and are they borne out by experimental data? Paul Leff and colleagues argue that accurate agonist affinity constants can be measured despite these predictions, but that effort must be made to detect any potential errors that might be anticipated from theory.

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