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Start Over Author "Moore, Amy G." Topic anti-inflammatory agents
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1. Identification and SAR of novel diaminopyrimidines. Part 1: The discovery of RO-4, a dual P2X3/P2X2/3 antagonist for the treatment of pain

Author

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., and Zhai, Yansheng

Subjects
*ANTI-inflammatory agents, *STRUCTURE-activity relationship in pharmacology, *PYRIMIDINES, *CHRONIC pain, *ION channels, *LIGANDS (Biochemistry), *DRUG derivatives
Abstract

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 optimization resulted in the discovery of RO-4, a potent, selective and drug-like dual P2X3/P2X2/3 antagonist. [Copyright &y& Elsevier]

Published
2009
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