(2,2‐Diphenyl‐[1,3]oxathiolan‐5‐ylmethyl)‐(3‐phenyl‐propyl)‐amine: a Potent and Selective 5‐HT1A Receptor Agonist期刊界 All Journals 搜尽天下杂志传播学术成果专业期刊搜索期刊信息化学术搜索

(2,2‐Diphenyl‐[1,3]oxathiolan‐5‐ylmethyl)‐(3‐phenyl‐propyl)‐amine: a Potent and Selective 5‐HT1A Receptor Agonist

Authors:	Silvia Franchini Dr Annalisa Tait Prof Adolfo Prandi Dr Claudia Sorbi Dr Rossella Gallesi Michela Buccioni Dr Gabriella Marucci Prof Carla De Stefani Dr Antonio Cilia Dr Livio Brasili Prof

Affiliation:	1. Dipartimento di Scienze Farmaceutiche, Università degli Studi di Modena e Reggio Emilia, Via Campi 183, 41100 Modena (Italy), Fax: (+39)?050‐205‐5131;2. Dipartimento di Scienze Chimiche, Università degli Studi di Camerino, Via S.?Agostino 1, 62032 Camerino (Italy);3. Divisione Ricerca e Sviluppo, Recordati S.p.A, Via Civitali 1, 20148 Milano (Italy)

Abstract:	A selective 5‐HT _1A receptor agonist : A new series of ligands acting at 5‐HT_1A serotonin receptor were identified. Among them (2,2‐diphenyl‐1,3]oxathiolan‐5‐yl‐methyl)‐(3‐phenyl‐propyl)amine (shown) possesses outstanding activity (pK_i=8.72, pD₂=7.67, E_max=85) and selectivity (5‐HT_1A/α_1D>150), and represents a new 5‐HT_1A agonist chemotype.

Keywords:	5‐HT1A biological activity drug design receptors structure– activity relationships