A single unified model for fitting simple to complex receptor response data.

ABSTRACT: The fitting of complex receptor-response data where fractional response and occupancy do not match is challenging. They encompass important cases including (a) the presence of "receptor reserve" and/or partial agonism, (b) multiple responses assessed at different vantage points along a pathway, (c) responses that are different along diverging downstream pathways (biased agonism), and (d) constitutive activity. For these, simple models such as the well-known Clark or Hill equations cannot be used. Those that can, such as the operational (Black&Leff) model, do not provide a unified approach, have multiple nonintuitive parameters that are challenging to fit in well-defined manner, have difficulties incorporating binding data, and cannot be reduced or connected to simpler forms. We have recent

SUBMITTER: Buchwald P 

PROVIDER: S-EPMC7414914 | biostudies-literature | 2020 Aug

REPOSITORIES: biostudies-literature