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

E M Naylor; 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

doi:10.1016/s0960-894x(98)00571-x

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.

Authors

E M Naylor¹, 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

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.

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