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.

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.

MeSH terms

  • Administration, Oral
  • Adrenergic beta-Agonists / administration & dosage*
  • Adrenergic beta-Agonists / chemical synthesis*
  • Adrenergic beta-Agonists / pharmacology*
  • Animals
  • Biological Availability
  • Dogs
  • Humans
  • Inhibitory Concentration 50
  • Kinetics
  • Rats
  • Sulfonamides / administration & dosage*
  • Sulfonamides / chemical synthesis*
  • Sulfonamides / pharmacology*
  • Tetrazoles / administration & dosage*
  • Tetrazoles / chemical synthesis*
  • Tetrazoles / pharmacology*

Substances

  • Adrenergic beta-Agonists
  • Sulfonamides
  • Tetrazoles
  • L 770644