2. Academic Validation
  3. L-770,644: a potent and selective human beta3 adrenergic receptor agonist with improved oral bioavailability

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

Affiliation

  • 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.

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