Abstract
The availability of recombinant receptors expressed in cell lines has allowed the detailed study of the interaction of ligands with receptors and receptors with their transduction processes. Such studies have indicated that for G protein-coupled receptors, agonists induce a conformational change in the receptor which promotes coupling to the G protein and hence G protein activation, whereas inverse agonists induce a conformational change which promotes G protein uncoupling and hence prevents G protein activation (1). It was further suggested that inverse agonists display a preferential affinity for the uncoupled state of the receptor (2). Recent studies have shown that heterologous expression systems expressing the 5-HT2C receptor display constitutive activity and that many compounds, such as mianserin, behave as inverse agonists (3).
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© 1997 Springer Science+Business Media New York
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Wood, M.D., Gager, T.L., Thomas, D.R., Holland, V.L., Brown, A.M. (1997). Antagonist Affinity Estimates from Radioligand Binding and Functional Studies Vary at the Cloned Human 5-HT2C Receptor. In: Teelken, A., Korf, J. (eds) Neurochemistry. Springer, Boston, MA. https://doi.org/10.1007/978-1-4615-5405-9_12
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DOI: https://doi.org/10.1007/978-1-4615-5405-9_12
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