| Literature DB >> 10201841 |
E R Parmee1, E M Naylor, L Perkins, V J Colandrea, H O Ok, M R Candelore, M A Cascieri, L Deng, W P Feeney, M J Forrest, G J Hom, D E MacIntyre, R R Miller, R A Stearns, C D Strader, L Tota, M J Wyvratt, M H Fisher, A E Weber.
Abstract
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.Entities:
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Year: 1999 PMID： 10201841 DOI： 10.1016/s0960-894x(99)00073-6
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823