2. Academic Validation
  3. 3-Pyridylethanolamines: potent and selective human beta 3 adrenergic receptor agonists

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

Affiliation

  • 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.

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