3-PYRIDYLETHANOLAMINES - POTENT AND SELECTIVE HUMAN BETA(3) ADRENERGIC-RECEPTOR AGONISTS

Authors
NAYLOR EM COLANDREA VJ CANDELORE MR CASCIERI MA COLWELL LF DENG LP FEENEY WP FORREST MJ HOM GJ MACINTYRE DE STRADER CD TOTA L WANG PR WYVRATT MJ FISHER MH WEBER AE
Citation
Em. Naylor et al., 3-PYRIDYLETHANOLAMINES - POTENT AND SELECTIVE HUMAN BETA(3) ADRENERGIC-RECEPTOR AGONISTS, Bioorganic & medicinal chemistry letters, 8(21), 1998, pp. 3087-3092
Citations number
15
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
8
Issue
21
Year of publication
1998
Pages
3087 - 3092
Database
ISI
SICI code
0960-894X(1998)8:21<3087:3-PASH>2.0.ZU;2-#
Abstract
The 3-pyridylethanolamine L-757,793 is a potent beta(3) AR agonist (EC 50 6.3 nM, 70% activation) with 1,300- and 500-fold selectivity over b inding to the beta(1) and beta(2) ARs, respectively. L-757,793 stimula ted lipolysis in rhesus monkeys (ED50 0.2 mg/kg) with a maximum respon se equivalent to that elicited by isoproterenol. (C) 1998 Elsevier Sci ence Ltd. All rights reserved.