3-Pyridylethanolamines: potent and selective human beta 3 adrenergic receptor agonists

Bioorg Med Chem Lett. 1998 Nov 3;8(21):3087-92. doi: 10.1016/s0960-894x(98)00571-x.

Abstract

The 3-pyridylethanolamine L-757,793 is a potent beta 3 AR agonist (EC50 6.3 nM, 70% activation) with 1,300- and 500-fold selectivity over binding to the beta 1 and beta 2 ARs, respectively. L-757,793 stimulated lipolysis in rhesus monkeys (ED50 0.2 mg/kg) with a maximum response equivalent to that elicited by isoproterenol.

MeSH terms

  • Adrenergic beta-Agonists / chemical synthesis*
  • Adrenergic beta-Agonists / pharmacology
  • Animals
  • Dogs
  • Humans
  • Macaca mulatta
  • Male
  • Receptors, Adrenergic, beta / drug effects*
  • Receptors, Adrenergic, beta-3
  • Structure-Activity Relationship
  • Sulfonamides / chemical synthesis*
  • Sulfonamides / pharmacology

Substances

  • Adrenergic beta-Agonists
  • L 755507
  • Receptors, Adrenergic, beta
  • Receptors, Adrenergic, beta-3
  • Sulfonamides