Discovery of P2X3 selective antagonists for the treatment of chronic pain

…, K Payza, N Popovic, D Projean, V Santhakumar…

文献索引：Cantin, Louis-David; Bayrakdarian, Malken; Buon, Christophe; Grazzini, Eric; Hu, Yun-Jin; Labrecque, Jean; Leung, Carmen; Luo, Xuehong; Martino, Giovanni; Pare, Michel; Payza, Kemal; Popovic, Nirvana; Projean, Denis; Santhakumar; Walpole, Christopher; Yu, Xiao Hong; Tomaszewski, Miroslaw J. Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 7 p. 2565 - 2571

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被引用次数: 13

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.