A critical re-evaluation of the slope factor of the operational model of agonism: When to exponentiate operational efficacy.

ABSTRACT: Agonist efficacy denoting the "strength" of agonist action is a cornerstone in the proper assessment of agonist selectivity and signalling bias. The simulation models are very accurate but complex and hard to fit experimental data. The parsimonious operational model of agonism (OMA) has become successful in the determination of agonist efficacies and ranking them. In 1983, Black and Leff introduced the slope factor to the OMA to make it more flexible and allow for fitting steep as well as flat concentration-response curves. First, we performed a functional analysis to indicate the potential pitfalls of the OMA. Namely, exponentiation of operational efficacy may break relationships among the OMA parameters. The fitting of the Black & Leff equation to the theoretical curves of several models

SUBMITTER: Randakova A 

PROVIDER: S-EPMC10579308 | biostudies-literature | 2023 Oct

REPOSITORIES: biostudies-literature