Quantitative pharmacological analysis of antagonist binding kinetics at CRF1 receptors in vitro and in vivo

BACKGROUND AND PURPOSE A series of novel non‐peptide corticotropin releasing factor type‐1 receptor (CRF1) antagonists were found to display varying degrees of insurmountable and non‐competitive behaviour in functional in vitro assays. We describe how we attempted to relate this behaviour to ligand receptor‐binding kinetics in a quantitative manner and how this resulted in the development and implementation of an efficient pharmacological screening method based on principles described by Motulsky and Mahan.

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