Characterization of three diaminopyrimidines as potent and selective antagonists of P2X3 and P2X2/3 receptors with in vivo efficacy in a pain model

British Journal of Pharmacology

Volumn 163, Issue 6, 2011, Pages 1315-1325

  Ballini, E ^a,c   Virginio, C ^a,c   Medhurst, S J ^b   Summerfield, S G ^b   Aldegheri, L ^a,c   Buson, A ^a,d   Carignani, C ^a,c   Chen, Y H ^b   Giacometti, A ^a,c   Lago, I ^a   Powell, A J ^b   Jarolimek, W ^a,d  

^a GSK   (Italy)

^b GLAXOSMITHKLINE   (United Kingdom)

^c Aptuit Inc   (United States)

^d Pharmaxis Ltd   (Australia)

Author keywords

antagonist; FLIPR; P2X; pain; patch clamp; purinergic

Indexed keywords

2,4 DIAMINOPYRIMIDINE DERIVATIVE; 5 [[4 CHLORO 5 METHYL 2 (1 METHYLETHYL)PHENYL]METHYL] 2,4 PYRIMIDINEDIAMINE; 5 [[4 CHLORO 5 METHYL 2 (1 METHYLETHYL)PHENYL]OXY] 2,4 PYRIMIDINEDIAMINE; 5 [[5 METHYL 2 (1 METHYLETHYL)PHENYL]OXY] 2,4 PYRIMIDINEDIAMINE; ANALGESIC AGENT; CALCIUM; PURINERGIC P2X1 RECEPTOR; PURINERGIC P2X2 RECEPTOR; PURINERGIC P2X3 RECEPTOR; PURINERGIC P2X4 RECEPTOR; PURINERGIC P2X7 RECEPTOR; PURINERGIC RECEPTOR BLOCKING AGENT; UNCLASSIFIED DRUG;

ANALGESIA; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; CALCIUM CELL LEVEL; CALCIUM TRANSPORT; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG EFFICACY; DRUG ELIMINATION; DRUG HALF LIFE; DRUG METABOLISM; DRUG TARGETING; ELECTROPHYSIOLOGY; HUMAN; HUMAN CELL; IC 50; IN VIVO STUDY; INFLAMMATORY PAIN; MALE; MAMMAL CELL; NEUROPATHIC PAIN; NONHUMAN; PAIN; PRIORITY JOURNAL; PROTEIN FUNCTION; RAT; RECEPTOR BLOCKING;

EID: 79959709453     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1111/j.1476-5381.2011.01322.x     Document Type: Article

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