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Mol Pharmacol 64:1271-1276, 2003

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Constitutive Activity and Inverse Agonists of G Protein-Coupled Receptors: a Current Perspective

Graeme Milligan

Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow, Scotland, United Kingdom

Over the last decade, the ability to detect agonist-independent signal transduction by G protein-coupled receptors has in turn resulted in the detection and study of ligands able to block this activity. Such ligands are generically described as inverse agonists. Considerable attention has recently been devoted to the presence and roles of endogenous antagonist/inverse agonists and the concept that inverse agonists may have specific therapeutic benefits compared with neutral antagonists.


Received June 20, 2003; accepted August 29, 2003

Address correspondence to: Graeme Milligan, Davidson Building, University of Glasgow, Glasgow G12 8QQ, Scotland, UK. E-mail: g.milligan{at}bio.gla.ac.uk




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