Discovery of a new series of 5-HT 1A receptor agonists

…, C Sorbi, A Tait, A Baraldi, P Angeli, M Buccioni…

Index: Franchini, Silvia; Prandi, Adolfo; Sorbi, Claudia; Tait, Annalisa; Baraldi, Annamaria; Angeli, Piero; Buccioni, Michela; Cilia, Antonio; Poggesi, Elena; Fossa, Paola; Brasili, Livio Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 6 p. 2017 - 2020

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Citation Number: 13

Abstract

Starting from compounds previously identified as α1-adrenoceptor antagonists that were also found to bind to the 5-HT1A receptor, in an attempt to separate the two activities, a new series of 5-HT1A receptor agonists was identified and shown to have high potency and/or high selectivity. Of these, compound 13, which combines high selectivity (5-HT1A/α1= 151) and good agonist potency (pD2= 7.82; Emax= 76), was found to be the most interesting.