Shih T L, Candelore M R, Cascieri M A, Chiu S H, Colwell L F, 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
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA.
Bioorg Med Chem Lett. 1999 May 3;9(9):1251-4. doi: 10.1016/s0960-894x(99)00182-1.
L-770,644 (9c) is a potent and selective agonist of the human beta3 adrenergic receptor (EC50 = 13 nM). It shows good oral bioavailability in both dogs and rats (%F = 27), and is a full agonist for glycerolemia in the rhesus monkey (ED50 = 0.21 mg/kg). Based on its desirable in vitro and in vivo properties, L-770,644 was chosen for further preclinical evaluation.
