期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 6, 页码 1628-1631出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.02.003
关键词
P2X3; Purinoceptors; ATP; RO-4; Chronic pain; Inflammatory pain; Neuropathic pain; Drug-like; P2X3 antagonist
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. (C) 2009 Elsevier Ltd. All rights reserved.
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