| Literature DB >> 19231180 |
David S Carter1, Muzaffar Alam, Haiying Cai, Michael P Dillon, Anthony P D W Ford, Joel R Gever, Alam Jahangir, Clara Lin, Amy G Moore, Paul J Wagner, Yansheng Zhai.
Abstract
P2X purinoceptors are ligand-gated ion channels whose endogenous ligand is ATP. Both the P2X(3) and P2X(2/3) receptor subtypes have been shown to play an important role in the regulation of sensory function and dual P2X(3)/P2X(2/3) 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 optimization resulted in the discovery of RO-4, a potent, selective and drug-like dual P2X(3)/P2X(2/3) antagonist.Entities:
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Year: 2009 PMID： 19231180 DOI： 10.1016/j.bmcl.2009.02.003
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823