On the importance of the "antagonist assumption" to how receptors express themselves.

Biochem Pharmacol

Department of Cellular Biochemistry, Glaxo Research Institute, Research Triangle Park, NC 27709, USA.

Published: June 1995

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http://dx.doi.org/10.1016/0006-2952(95)00137-oDOI Listing

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"Phenotypic" pharmacology: the influence of cellular environment on G protein-coupled receptor antagonist and inverse agonist pharmacology.

Biochem Pharmacol

March 2007

Department of Cell Physiology & Pharmacology, University of Leicester, Henry Wellcome Building, Lancaster Road, Leicester LE1 9HN, UK.

A central dogma of G protein-coupled receptor (GPCR) pharmacology has been the concept that unlike agonists, antagonist ligands display equivalent affinities for a given receptor, regardless of the cellular environment in which the affinity is assayed. Indeed, the widespread use of antagonist pharmacology in the classification of receptor expression profiles in vivo has relied upon this 'antagonist assumption'. However, emerging evidence suggests that the same gene-product may exhibit different antagonist pharmacological profiles, depending upon the cellular context in which it is expressed-so-called 'phenotypic' profiles.

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