Human beta3 adrenergic receptor agonists containing imidazolidinone and imidazolone benzenesulfonamides.
作者信息
Naylor E M, Parmee E R, Colandrea V J, Perkins L, Brockunier L, Candelore M R, Cascieri M A, Colwell L F, Deng L, Feeney W P, Forrest M J, Hom G J, MacIntyre D E, Strader C D, Tota L, Wang P R, 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):755-8. doi: 10.1016/s0960-894x(99)00072-4.
Abstract
The cyclopentylpropylimidazolidinone L-766,892 is a potent beta3 AR agonist (EC50 5.7 nM, 64% activation) with 420- and 130-fold selectivity over binding to the beta1 and beta2 ARs, respectively. In anesthetized rhesus monkeys, L-766,892 elicited dose-dependent hyperglycerolemia (ED50 0.1 mg/kg) with minimal effects on heart rate.
摘要
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