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.
E M Naylor  1 ,  V J Colandrea ,  M R Candelore ,  M A Cascieri ,  L F Colwell Jr ,  L Deng ,  W P Feeney ,  M J Forrest ,  G J Hom ,  D E MacIntyre ,  C D Strader ,  L Tota ,  P R Wang ,  M J Wyvratt ,  M H Fisher ,  A E Weber
Affiliations
  • 1. Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, New Jersey 07065, USA.
PMID: 9873681 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.