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Molecular Interventions 4:326-336, (2004)
© American Society for Pharmacology and Experimental Therapeutics
10.1124/mi.4.6.6
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Review

The Receptor Concept: A Continuing Evolution

Lee E. Limbird

Department of Pharmacology and Center for Molecular Neuroscience, Vanderbilt University School of Medicine, and Vanderbilt Kennedy Center for Research on Human Development, Nashville, Tennessee 37232


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This review briefly summarizes the development of the receptor concept, the identification of receptors based first on biological response data and subsequently on radioligand binding properties, and the biological and physiological understandings that these approaches have made possible. The development of receptor characterization began with receptors that ultimately were discovered to mediate response by coupling to G-binding proteins, also known as G protein–coupled receptors (GPCRs). Consequently, many if not all of the examples in this overview will describe studies characterizing GPCRs in general, and adrenergic receptors in particular. The purpose of this review, however, is not a detailed chronological account of a huge literature, but rather an overview of the fundamental questions posed and answered by these studies.




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Copyright © 2004 by the American Society for Pharmacology and Experimental Therapeutics.