5-HT1A and 5-HT2A ligands with anxiolytic and antipanic-like properties

被引：17
|
作者：
Diouf, O
Carato, P
Depreux, P
Bonte, JP
Caignard, DH
GuardiolaLemaitre, B
Rettori, MC
Belzung, C
Lesieur, D
机构：
[1] INST CHIM PHARMACEUT, F-59006 LILLE, FRANCE
[2] ADIR, F-92415 COURBEVOIE, FRANCE
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 20期
关键词：
D O I：
10.1016/S0960-894X(97)10023-3
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of new benzothiazolin-2-one, benzoxazolin-2-one and benzoxazin-3-one derivatives were synthesized and their binding profile at 5-HT1A, 5-HT2A, 5-HT2C as well as D-2 and alpha(1) receptors was determined. All studied compounds displayed high to moderate affinity for both 5-HT1A and 5-HT2A receptor subtypes. Among these, one compound (29) emerged since it exhibited potent antagonist activities at 5-HT1A, 5-HT2A, D-2 and alpha(1) central receptors and showed anxiolytic and antipanic-like effects in mice. 29 is currently undergoing preclinical evaluation. (C) 1997 Elsevier Science Ltd.
引用
收藏
页码：2579 / 2584
页数：6
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