Human β3 adrenergic receptor agonists containing cyanoguanidine and nitroethylenediamine moieties

被引：15

作者：

Brockunier, LL

Candelore, MR

Cascieri, MA

Liu, Y

Tota, L

Wyvratt, MJ

Fisher, MH

Weber, AE

Parmee, ER ^{[1
]}

机构：

[1] Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA

[2] Merck Res Labs, Dept Biochem, Rahway, NJ 07065 USA

[3] Merck Res Labs, Dept Physiol, Rahway, NJ 07065 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 03期

关键词：

D O I：

10.1016/S0960-894X(00)00669-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Pyridineethanolamine derivatives containing cyanoguanidine or nitroethylenediamine moieties were examined as human Bi adrenergic receptor (AR) agonists. Notably, indoline derivatives 6a and 11 were potent beta (3) AR agonists (beta (3) EC50 = 13 and 19 nM, respectively), which showed good selectivity over binding to and minimal activation of the beta (1) and beta (2) ARs. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：379 / 382

页数：4

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