Receptor localization, native tissue binding and ex vivo occupancy for centrally penetrant P2X7 antagonists in the rat

British Journal of Pharmacology

Volumn 162, Issue 2, 2011, Pages 405-414

  Able, S L ^a   Fish, R L ^a   Bye, H ^a,b   Booth, L ^a   Logan, Y R ^a   Nathaniel, C ^a   Hayter, P ^a   Katugampola, S D ^a  

^a PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United Kingdom)

^b KING'S COLLEGE LONDON   (United Kingdom)

Author keywords

occupancy; P2X7 receptor; radioligand binding; rat cortex

Indexed keywords

2 CYANO 1 [(1S) 1 PHENYLETHYL] 3 QUINOLIN 5 YLGUANIDINE; 3 [1 (2 CHLORO 3 TRIFLUOROMETHYLPHENYL) 1H TETRAZOL 5 YLMETHYL]PYRIDINE; [1 [[(CYANOIMINO)(5 QUINOLINYLAMINO)METHYL]AMINO] 2,2 DIMETHYLPROPYL] 2 (3,4 DIMETHOXYPHENYL)ACETAMIDE; A 740003; A 804598; PURINERGIC P2X7 RECEPTOR; PURINERGIC P2X7 RECEPTOR ANTAGONIST; PURINERGIC RECEPTOR BLOCKING AGENT; RADIOLIGAND; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; AUTORADIOGRAPHY; BINDING AFFINITY; BINDING KINETICS; BRAIN CORTEX; CONTROLLED STUDY; DOSE RESPONSE; EX VIVO STUDY; GRAY MATTER; IN VITRO STUDY; LIGAND BINDING; MALE; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; PROTEIN LOCALIZATION; RAT; RECEPTOR BINDING; RECEPTOR OCCUPANCY; SPINAL CORD; TISSUE HOMOGENATE;

ANIMALS; AUTORADIOGRAPHY; BINDING, COMPETITIVE; BRAIN; CEREBRAL CORTEX; DRUG DISCOVERY; GUANIDINES; MALE; MOLECULAR TARGETED THERAPY; PROTEIN BINDING; PURINERGIC P2X RECEPTOR ANTAGONISTS; QUINOLINES; RADIOLIGAND ASSAY; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, PURINERGIC P2X7; SPINAL CORD;

EID: 78650325255     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1111/j.1476-5381.2010.01025.x     Document Type: Article

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