L-770,644: a potent and selective human beta3 adrenergic receptor agonist with improved oral bioavailability

  • Bioorg Med Chem Lett. 1999 May 3;9(9):1251-4. doi: 10.1016/s0960-894x(99)00182-1.
T L Shih  1 ,  M R Candelore ,  M A Cascieri ,  S H Chiu ,  L F Colwell Jr ,  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
Affiliations
  • 1. Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA.
PMID: 10340609 DOI: 10.1016/s0960-894x(99)00182-1
Abstract

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.

Products