DISCOVERY OF L-755,507 - A SUBNANOMOLAR HUMAN BETA(3) ADRENERGIC-RECEPTOR AGONIST

Authors
PARMEE ER OK HO CANDELORE MR TOTA L DENG LP STRADER CD WYVRATT MJ FISHER MH WEBER AE
Citation
Er. Parmee et al., DISCOVERY OF L-755,507 - A SUBNANOMOLAR HUMAN BETA(3) ADRENERGIC-RECEPTOR AGONIST, Bioorganic & medicinal chemistry letters, 8(9), 1998, pp. 1107-1112
Citations number
8
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
8
Issue
9
Year of publication
1998
Pages
1107 - 1112
Database
ISI
SICI code
0960-894X(1998)8:9<1107:DOL-AS>2.0.ZU;2-0
Abstract
A study of 4-acylaminobenzenesulfonamides in a cloned human beta(3) ad renergic receptor assay resulted in the discovery of n-hexylurea, L-75 5,507 (22). This 0.43 nM beta(3) agonist, which is > 440-fold selectiv e over both beta(1) and beta(2) binding, is among the most potent huma n beta(3) agonists reported to date. (C) 1998 Elsevier Science Ltd. Al l rights reserved.