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Discovery of P2X3 selective antagonists for the treatment of chronic pain
Authors:Cantin Louis-David  Bayrakdarian Malken  Buon Christophe  Grazzini Eric  Hu Yun-Jin  Labrecque Jean  Leung Carmen  Luo Xuehong  Martino Giovanni  Paré Michel  Payza Kemal  Popovic Nirvana  Projean Denis  Santhakumar V  Walpole Christopher  Yu Xiao Hong  Tomaszewski Mirosław J
Affiliation:Department of Medicinal Chemistry, AstraZeneca R&D, 7171 Frederick-Banting, Montréal, QC, Canada H4S 1Z9. Louis-david.cantin@astrazeneca.com
Abstract: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.
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