Human β3 adrenergic receptor agonists containing imidazolidinone and imidazolone benzenesulfonamides

被引：45

作者：

Naylor, EM ^{[1
]}

Parmee, ER

Colandrea, VJ

Perkins, L

Brockunier, L

Candelore, MR

Cascieri, MA

Colwell, LF

Deng, LP

Feeney, WP

Forrest, MJ

Hom, GJ

MacIntyre, DE

Strader, CD

Tota, L

Wang, PR

Wyvratt, MJ

Fisher, MH

Weber, AE

机构：

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

[2] Merck Res Labs, Dept Mol Pharmacol Immunol & Rheumatol, Rahway, NJ 07065 USA

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

[4] Merck Res Labs, Lab Anim Resources, Rahway, NJ 07065 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 05期

关键词：

D O I：

10.1016/S0960-894X(99)00072-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The cyclopentylpropylimidazolidinone L-766,892 is a potent beta(3) AR agonist (EC50 5.7 nM, 64% activation) with 420- and 130-fold selectivity over binding to the beta(1) and beta(2) ARs, respectively. In anesthetized rhesus monkeys, L-766,892 elicited dose-dependent hyperglycerolemia (ED50 0.1 mg/kg) with minimal effects on heart rate. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：755 / 758

页数：4

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