High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity

…, JM Autin, P Funes, A Newman-Tancredi…

Index: Maurel, Jean Louis; Autin, Jean-Marie; Funes, Philippe; Newman-Tancredi, Adrian; Colpaert, Francis; Vacher, Bernard Journal of Medicinal Chemistry, 2007 , vol. 50, # 20 p. 5024 - 5033

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Citation Number: 47

Abstract

We report the discovery of novel 5-HT1A receptor agonists and describe the process that led to the antidepressant candidate 9 (F 15599). 9 has nanomolar affinity for 5-HT1A binding sites and is over 1000-fold selective with respect to the other 5-HT1 receptor subtypes, 5- HT2-7 receptor families, and also numerous GPCRs, transporters, ion channels, and enzymes. In a cellular model of signal transduction, 9 activates h5-HT1A receptors with an ...