Novel arylpiperazines as selective alpha(1)-adrenergic receptor antagonists

Authors
Li, XB Murray, WV Jolliffe, L Pulito, V
Citation
Xb. Li et al., Novel arylpiperazines as selective alpha(1)-adrenergic receptor antagonists, BIOORG MED, 10(10), 2000, pp. 1093-1096
Citations number
4
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
10
Year of publication
2000
Pages
1093 - 1096
Database
ISI
SICI code
0960-894X(20000515)10:10<1093:NAASAR>2.0.ZU;2-E
Abstract
A novel series of arylpiperazines has been synthesized and identified as an tagonists of alpha(1a) adrenergic receptor (alpha(1a)-AR) implicated in ben ign prostatic hyperplasia. These compounds selectively bind to membrane bou nd alpha(1a)-AR with K(i)s as low as 0.66 nM. As such, these potentially re present a viable treatment for BPH without the side effects associated with known alpha(1)-adrenergic antagonists. (C) 2000 Elsevier Science Ltd. All rights reserved.