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Discovery of P2X3 selective antagonists for the treatment of chronic pain |
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| 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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