Novel and potent human and rat β3-adrenergic receptor agonists containing substituted 3-indolylalkylamines

被引：45

作者：

Harada, H

Hirokawa, Y

Suzuki, K

Hiyama, Y

Oue, M

Kawashima, H

Yoshida, N

Furutani, Y

Kato, S

机构：

[1] Dainippon Pharmaceut Co Ltd, Chem Res Labs, Suita, Osaka 5640053, Japan

[2] Dainippon Pharmaceut Co Ltd, Pharmacol & Microbiol Res Labs, Suita, Osaka 5640053, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 07期

关键词：

D O I：

10.1016/S0960-894X(03)00073-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of 2-(3-indolyl)alkylamino-1-(3-chlorophenyl)ethanois was prepared and evaluated for in vitro ability to stimulate cAMP production in Chinese hamster ovary cells expressing cloned human beta(3)-AR. The optically active 30a was found to be the most potent and selective human beta(3)-AR agonist in this series with an EC50 value of 0.062 nM. In addition, 30a selectivity for human beta(3)-AR was 210-fold and 103-fold that for human beta(2)-AR and beta(1)-AR, respectively. Furthermore, 30a showed potent agonistic activity at rat beta(3)-AR. (C) 2003 Elsevier Science Ltd. All rights reserved.

引用

页码：1301 / 1305

页数：5

共 28 条

[1] THE BROWN ADIPOCYTE BETA-ADRENOCEPTOR [J].