Human Beta(3) Adrenergic Receptor Agonists Containing Cyclic Ureidobenzenesulfonamides

Emma R. Parmee,Elizabeth M. Naylor,Leroy Perkins,Vincent J. Colandrea,Hyun O. Ok,Mari R. Candelore,Margaret A. Cascieri,Liping Deng,William P. Feeney,Michael J. Forrest,Gary J. Hom,D.Euan MacIntyre,Randall R. Miller,Ralph A. Stearns,Catherine D. Strader,Laurie Tota,Matthew J. Wyvratt,Michael H. Fisher,Ann E. Weber

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS（1999）

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摘要

Human beta(3) adrenergic receptor agonists containing 5-membered ring ureas were shown to be potent partial agonists with excellent selectivity over beta(1) and beta(2) binding. L-760,087 (4a) and L-764,646 (5a) (beta(3) EC50 = 18 and 14 nM, respectively) stimulate lipolysis in rhesus monkeys (ED50 = 0.2 and 0.1 mg/kg, respectively) with minimal effects on heart rate. Oral absorption in dogs is improved over other urea analogs. (C) 1999 Elsevier Science Ltd. All rights reserved.

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