Human beta3 adrenergic receptor agonists containing cyclic ureidobenzenesulfonamides.

作者信息

Parmee E R, Naylor E M, Perkins L, Colandrea V J, Ok H O, Candelore M R, Cascieri M A, Deng L, Feeney W P, Forrest M J, Hom G J, MacIntyre D E, Miller R R, Stearns R A, Strader C D, Tota L, Wyvratt M J, Fisher M H, Weber A E

机构信息

Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA.

出版信息

Bioorg Med Chem Lett. 1999 Mar 8;9(5):749-54. doi: 10.1016/s0960-894x(99)00073-6.

Human beta3 adrenergic receptor agonists containing 5-membered ring ureas were shown to be potent partial agonists with excellent selectivity over beta1 and beta2 binding. L-760,087 (4a) and L-764,646 (5a) (beta3 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.