Identification and SAR of novel diaminopyrimidines. Part 1: The discovery of RO-4, a dual P2X3/P2X2/3 antagonist for the treatment of pain

Bioorganic and Medicinal Chemistry Letters

Volumn 19, Issue 6, 2009, Pages 1628-1631

  Carter, David S ^a   Alam, Muzaffar ^a   Cai, Haiying ^a   Dillon, Michael P ^a   Ford, Anthony P D W ^a   Gever, Joel R ^a   Jahangir, Alam ^a   Lin, Clara ^a   Moore, Amy G ^a   Wagner, Paul J ^a   Zhai, Yansheng ^a  

^a ROCHE BIOSCIENCE   (United States)

Author keywords

ATP; Chronic pain; Drug like; Inflammatory pain; Neuropathic pain; P2X3; P2X3 antagonist; Purinoceptors; RO 4

Indexed keywords

ALDEHYDE; DIAMINOPYRIMIDINE DERIVATIVE; POLYCYCLIC AROMATIC HYDROCARBON DERIVATIVE; PURINERGIC P2X2 RECEPTOR; PURINERGIC P2X3 RECEPTOR; PURINERGIC RECEPTOR BLOCKING AGENT; PYRIMIDINE DERIVATIVE; RO 4; TRIMETHOPRIM; UNCLASSIFIED DRUG;

ALKYLATION; ANIMAL CELL; ARTICLE; CONTROLLED STUDY; DRUG IDENTIFICATION; DRUG STRUCTURE; HUMAN; HUMAN CELL; HYDROPHOBICITY; IC 50; NONHUMAN; PROTEIN BINDING; PROTEIN FUNCTION; STRUCTURE ACTIVITY RELATION;

ADENOSINE TRIPHOSPHATE; ANALGESICS; CHEMISTRY, PHARMACEUTICAL; DRUG DESIGN; DRUG EVALUATION, PRECLINICAL; HUMANS; INHIBITORY CONCENTRATION 50; IONS; LIGANDS; MODELS, CHEMICAL; PAIN; PYRIMIDINES; RECEPTORS, PURINERGIC P2; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 61349100301     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.02.003     Document Type: Article

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