Yohimbine dimers exhibiting binding selectivities for human alpha(2a)- versus alpha(2b)-adrenergic receptors

Authors
Zheng, WP Lei, LP Lalchandani, S Sun, GP Feller, DR Miller, DD
Citation
Wp. Zheng et al., Yohimbine dimers exhibiting binding selectivities for human alpha(2a)- versus alpha(2b)-adrenergic receptors, BIOORG MED, 10(7), 2000, pp. 627-630
Citations number
41
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
7
Year of publication
2000
Pages
627 - 630
Database
ISI
SICI code
0960-894X(20000403)10:7<627:YDEBSF>2.0.ZU;2-5
Abstract
A series of yohimbine dimers was prepared and evaluated at the human alpha( 2a)- and alpha(2b)-adrenergic receptors (ARs) expressed in Chinese hamster ovary (CHO) cells. All dimers display higher binding selectivities for alph a(2a) versus alpha(2b) subtype than yohimbine, and four compounds (3d, 3e, 3g and 3i) represent the most potent and alpha(2a)- versus alpha(2b)-AR sel ective ligands identified so far. (C) 2000 Elsevier Science Ltd. All rights reserved.