Identification and SAR of novel diaminopyrimidines. Part 1: The discovery of RO-4, a dual P2X 3/P2X 2/3 antagonist for the treatment of pain

…, A Jahangir, C Lin, AG Moore, PJ Wagner…

Index: Carter, David S.; Alam, Muzaffar; Cai, Haiying; Dillon, Michael P.; Ford, Anthony P.D.W.; Gever, Joel R.; Jahangir, Alam; Lin, Clara; Moore, Amy G.; Wagner, Paul J.; Zhai, Yansheng Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 6 p. 1628 - 1631

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Citation Number: 39

Abstract

P2X purinoceptors are ligand-gated ion channels whose endogenous ligand is ATP. Both the P2X3 and P2X2/3 receptor subtypes have been shown to play an important role in the regulation of sensory function and dual P2X3/P2X2/3 antagonists offer significant potential for the treatment of pain. A high-throughput screen of the Roche compound collection resulted in the identification of a novel series of diaminopyrimidines; subsequent ...