Discovery of P2X3 selective antagonists for the treatment of chronic pain

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• 作者：Louis-David Cantin^a ; ^{Louis-david.cantin@astrazeneca.com} ; ^{ldcantin@eckerdalumni.com} ; Malken Bayrakdarian^a ; Christophe Buon^a ; Eric Grazzini^c ; Yun-Jin Hu^a ; Jean Labrecque^c ; Carmen Leung^a ; Xuehong Luo^a ; Giovanni Martino^c ; Michel Paré ; ^c ; Kemal Payza^c ; Nirvana Popovic^a ; Denis Projean^b ; V. Santhakumar^a ; Christopher Walpole^a ; Xiao Hong Yu^c ; Miros艂aw J. Tomaszewski^a
• 关键词：P2X3 ; Purinergic receptors ; Analgesia ; Pyrrolo-pyrimidinones ; Nociceptive pain
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：1 April, 2012
• 卷：22
• 期：7
• 页码：2565-2571
• 文件大小：950 K

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.