Benzodiazepine binding site occupancy by the novel GABAA receptor subtype-selective drug 7-(1,1-dimethylethyl)-6-(2-ethyl-2H-1,2,4- triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine (TPA023) in rats, primates, and humans

Journal of Pharmacology and Experimental Therapeutics

Volumn 332, Issue 1, 2010, Pages 17-25

  Atack, John R ^a,e   Wong, Dean F ^b   Fryer, Tim D ^c   Ryan, Christine ^d   Sanabria, Sandra ^d   Zhou, Yun ^b   Dannals, Robert F ^b   Eng, Wai Si ^d   Gibson, Raymond E ^d   Burns, H Donald ^d   Vega, Jose M ^d,f   Vessy, Laura ^d   Scott Stevens, Paul ^a,g   Beech, John S ^c   Baron, Jean Claude ^c   Sohal, Bindi ^a,h   Schrag, Michael L ^d   Aigbirhio, Franklin I ^c   McKernan, Ruth M ^a,i   Hargreaves, Richard J ^d  

^a NEUROSCIENCE RESEARCH CENTRE   (United Kingdom)

^b DEPARTMENT OF PATHOLOGY   (United States)

^c UNIVERSITY OF CAMBRIDGE   (United Kingdom)

^d MERCK RESEARCH LABORATORIES   (United States)

^e JANSSEN RESEARCH AND DEVELOPMENT   (Belgium)

^f AMGEN INC   (United States)

^g GLAXOSMITHKLINE   (United Kingdom)

^h NOVARTIS   (United Kingdom)

ⁱ PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

4 AMINOBUTYRIC ACID A RECEPTOR; 7 (1,1 DIMETHYLETHYL) 6 (2 ETHYL 2H 1,2,4 TRIAZOL 3 YLMETHOXY) 3 (2 FLUOROPHENYL) 1,2,4 TRIAZOLO[4,3 B]PYRIDAZINE; BENZODIAZEPINE; FLUMAZENIL C 11; FLUMAZENIL H 3; IOMAZENIL I 123; PYRIDAZINE; RADIOPHARMACEUTICAL AGENT; TPA 023; UNCLASSIFIED DRUG;

ADULT; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BABOON; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; FEMALE; GAMMA SCINTIGRAPHY; HUMAN; HUMAN EXPERIMENT; HUMAN VERSUS ANIMAL COMPARISON; IN VIVO STUDY; LOW DRUG DOSE; MALE; NONHUMAN; NORMAL HUMAN; POSITRON EMISSION TOMOGRAPHY; PRIMATE; PRIORITY JOURNAL; RAT; RECEPTOR OCCUPANCY; RHESUS MONKEY; SEDATION; SPECIES;

ANIMALS; BINDING SITES; BRAIN; DOSE-RESPONSE RELATIONSHIP, DRUG; FLUMAZENIL; GABA AGONISTS; HUMANS; MACACA MULATTA; PAPIO; POSITRON-EMISSION TOMOGRAPHY; PROTEIN BINDING; PROTEIN SUBUNITS; PYRIDAZINES; RADIOLIGAND ASSAY; RATS; RECEPTORS, GABA-A; SPECIES SPECIFICITY; TISSUE DISTRIBUTION; TRIAZOLES;

EID: 73949159504     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.109.157909     Document Type: Article

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