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

被引：15

作者：

Franchini, Silvia ^{[1
]}

Tait, Annalisa ^{[1
]}

Prandi, Adolfo ^{[1
]}

Sorbi, Claudia ^{[1
]}

Gallesi, Rossella ^{[1
]}

Buccioni, Michela ^{[2
]}

Marucci, Gabriella ^{[2
]}

De Stefani, Carla ^{[3
]}

Cilia, Antonio ^{[3
]}

Brasili, Livio ^{[1
]}

机构：

[1] Univ Modena & Reggio Emilia, Dipartimento Sci Farmaceut, I-41100 Modena, Italy

[2] Univ Camerino, Dipartimento Sci Chim, I-62032 Camerino, Italy

[3] Recordati SpA, Div Ric & Sviluppo, I-20148 Milan, Italy

来源：

CHEMMEDCHEM | 2009年 / 4卷 / 02期

关键词：

5-HT1A; biological activity; drug design; receptors; structure-activity relationships; LIGANDS; ACETYLCHOLINE; ANTAGONISTS; SEROTONIN; RATS;

D O I：

10.1002/cmdc.200800276

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Starting from compound 1, a previously reported alpha(1D)-adrenoceptors antagonist, a new series of ligands acting at 5-HT1A serotonin receptor were identified through simple structure modifications. Among them (2,2-diphenyl-[1,3]oxothiolon-5-yl-methyl)-(3-phenyl-propyl)amine (79) exhibits outstanding activity (pK(1) = 8.72, pD(2) = 7.67, E-max = 85) and selectivity (5-HT1A/alpha(1D) > 150), and represents an as yet unidentified 5-HT1A agonist scaffold.

引用

页码：196 / 203

页数：8

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