Discovery of P2X3 selective antagonists for the treatment of chronic pain

作者:Cantin Louis David*; Bayrakdarian Malken; Buon Christophe; Grazzini Eric; Hua Yun Jin; Labrecque Jean; Leung Carmen; Luo Xuehong; Martino Giovanni; Pare Michel; Payza Kemal; Popovic Nirvana; Projean Denis; Santhakumar V; Walpole Christopher; Yu Xiao Hong; Tomaszewski Miroslaw J
来源:Bioorganic & Medicinal Chemistry Letters, 2012, 22(7): 2565-2571.
DOI:10.1016/j.bmcl.2012.01.124

摘要

Purinergic receptor P2X3 has been linked to analgesia in a number of pre-clinical models of pain, and is expressed in the human pain perception pathway. Only few P2X3-selective antagonists have been reported to date. This Letter describes the SAR and in vivo analgesic profile of a novel scaffold of selective P2X3 antagonists.

  • 出版日期2012-4-1