Novel arylpiperazines as selective α 1-adrenergic receptor antagonists

X Li, WV Murray, L Jolliffe, V Pulito

Index: Li, Xiaobing; Murray, William V.; Jolliffe, Linda; Pulito, Virginia Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 10 p. 1093 - 1096

Full Text: HTML

Citation Number: 10

Abstract

A novel series of arylpiperazines has been synthesized and identified as antagonists of α1a adrenergic receptor (α1a-AR) implicated in benign prostatic hyperplasia. These compounds selectively bind to membrane bound α1a-AR with Kis as low as 0.66 nM. As such, these potentially represent a viable treatment for BPH without the side effects associated with known α1-adrenergic antagonists.