3-pyridylethanolamines: Potent and selective human β3 adrenergic receptor agonists
作者:Elizabeth M. Naylor、Vincent J. Colandrea、Mari R. Candelore、Margaret A. Cascieri、Lawrence F. Colwell、Liping Deng、William P. Feeney、Michael J. Forrest、Gary J. Hom、D. Euan MacIntyre、Catherine D. Strader、Laurie Tota、Pei-Ran Wang、Matthew J. Wyvratt、Michael H. Fisher、Ann E. Weber
DOI:10.1016/s0960-894x(98)00571-x
日期:1998.11
The 3-pyridylethanolamine L-757,793 is a potent beta(3) AR agonist (EC50 6.3 nM, 70% activation) with 1,300- and 500-fold selectivity over binding to the beta(1) and beta(2) ARs, respectively. L-757,793 stimulated lipolysis in rhesus monkeys (ED50 0.2 mg/kg) with a maximum response equivalent to that elicited by isoproterenol. (C) 1998 Elsevier Science Ltd. All rights reserved.