Identification and SAR of novel diaminopyrimidines. Part 2: The discovery of RO-51, a potent and selective, dual P2X3/P2X2/3 antagonist for the treatment of pain

Bioorganic and Medicinal Chemistry Letters

Volumn 19, Issue 6, 2009, Pages 1632-1635

  Jahangir, Alam ^a   Alam, Muzaffar ^a   Carter, David S ^a   Dillon, Michael P ^a   Bois, Daisy Joe Du ^a   Ford, Anthony P D W ^a   Gever, Joel R ^a   Lin, Clara ^a   Wagner, Paul J ^a   Zhai, Yansheng ^a   Zira, Jeff ^a  

^a ROCHE BIOSCIENCE   (United States)

Author keywords

ATP; Diaminopyrimidine; Neuropathic pain; P2X2 3; P2X3 P2X2 3; Purinoceptor; RO 4; RO 51

Indexed keywords

AMINE; AMINO ACID; DIAMINOPYRIMIDINE DERIVATIVE; PURINERGIC P2X2 RECEPTOR; PURINERGIC P2X3 RECEPTOR; PURINERGIC RECEPTOR BLOCKING AGENT; PYRIMIDINE DERIVATIVE; RO 4; RO 51; UNCLASSIFIED DRUG;

AMINO ACID SUBSTITUTION; ANIMAL CELL; ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DRUG CLEARANCE; DRUG HALF LIFE; DRUG INHIBITION; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; HYDROGENATION; IC 50; NONHUMAN; PAIN; RAT; RECEPTOR AFFINITY; SINGLE DRUG DOSE; STRUCTURE ACTIVITY RELATION;

ADENOSINE TRIPHOSPHATE; ANALGESICS; ANIMALS; CHEMISTRY, PHARMACEUTICAL; CHO CELLS; CRICETINAE; CRICETULUS; DRUG DESIGN; DRUG EVALUATION, PRECLINICAL; HUMANS; INHIBITORY CONCENTRATION 50; MODELS, CHEMICAL; PAIN; PYRIMIDINES; RECEPTORS, PURINERGIC P2; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 61349092411     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.01.097     Document Type: Article

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