Development of a presynaptic 5-HT1A antagonist

被引：17

作者：

Mattson, RJ

Catt, JD

Sloan, CP

Gao, Q

Carter, RB

Gentile, A

Mahle, CD

Matos, FF

McGovern, R

VanderMaelen, CP

Yocca, FD

机构：

[1] Bristol Myers Squibb Co, Pharmaceut Res Inst, Wallingford, CT 06492 USA

[2] CoCensys Inc, Irvine, CA 92718 USA

[3] Bayer Pharmaceut Res Ctr, West Haven, CT USA

[4] Pfizer Global Res & Dev, Groton, CT USA

[5] Boehringer Ingelheim Pharmaceut Inc, Ridgefield, CT 06877 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 02期

关键词：

D O I：

10.1016/S0960-894X(02)00879-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new 5-HT1A silent antagonist 14 (5-HT1A IC50 = 2.2 nM) antagonizes the effects of agonists on reciprocal forepaw treading behavior, on neuronal firing in the rat dorsal raphe, and on 5-HT1A release in the raphe and hippocampus. While 14 alone was inactive in the social interaction paradigm, it completely reversed the social interaction activity of the serotonergic compounds (buspirone, 1, and 2). (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：285 / 288

页数：4

共 23 条

[1] BEHAVIORAL AND BIOCHEMICAL-EVIDENCE OF THE INTERACTION OF THE PUTATIVE ANTIPSYCHOTIC AGENT, BMY-14802 WITH THE 5-HT1A RECEPTOR [J].