Preclinical and clinical pharmacology of TPA023B, a GABAA receptor α2/α3 subtype-selective partial agonist

Journal of Psychopharmacology

Volumn 25, Issue 3, 2011, Pages 329-344

  Atack, J R ^a   Hallett, D J ^a   Tye, S ^a   Wafford, K A ^a   Ryan, C ^b   Sanabria Bohorquez S M ^b   Eng, Wai Si ^b   Gibson, R E ^b   Burns, H D ^b   Dawson, G R ^a   Carling, R W ^a   Street, L J ^a   Pike, A ^a   De Lepeleire, I ^c   Van Laere, K ^d   Bormans, G ^d   De Hoon, J N ^d   Van Hecken, A ^d   McKernan, R M ^a   Murphy, M G ^b   Hargreaves, R J ^b   more..

^a NEUROSCIENCE RESEARCH CENTRE   (United Kingdom)

^b MERCK RESEARCH LABORATORIES   (United States)

^c Merck Sharp and Dohme   (Belgium)

^d UNIVERSITY OF LEUVEN   (Belgium)

Author keywords

benzodiazepine; GABAA receptor; non sedating anxiolytic; subtype selective

Indexed keywords

4 AMINOBUTYRIC ACID A RECEPTOR ALPHA2; 4 AMINOBUTYRIC ACID A RECEPTOR ALPHA3; 4 AMINOBUTYRIC ACID A RECEPTOR STIMULATING AGENT; 6,2' DIFLUORO 5' [3 (1 HYDROXY 1 METHYLETHYL)IMIDAZO(1,2 B)(1,2,4)TRIAZIN 7 YL]BIPHENYL 2 CARBONITRILE; ANXIOLYTIC AGENT; CHLORDIAZEPOXIDE; DIAZEPAM; FLUMAZENIL C 11; TPA 023B; UNCLASSIFIED DRUG;

ADULT; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANXIETY DISORDER; AREA UNDER THE CURVE; ARTICLE; ATAXIA; BINDING AFFINITY; BINDING ASSAY; BRAIN; CLINICAL PHARMACOLOGY; CONTROLLED STUDY; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG EFFICACY; DRUG HALF LIFE; DRUG SAFETY; DRUG TOLERABILITY; EMOTIONALITY; FATIGUE; HUMAN; HUMAN CELL; MALE; MAXIMUM PLASMA CONCENTRATION; MAXIMUM TOLERATED DOSE; MAZE TEST; MOUSE; MUSCLE RELAXATION; NONHUMAN; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; PSYCHOPHARMACOLOGY; RAT; RODENT; SEDATION; SINGLE DRUG DOSE; SOMNOLENCE; SQUIRREL MONKEY; TIME TO MAXIMUM PLASMA CONCENTRATION; TRANQUILIZING ACTIVITY; TREATMENT RESPONSE;

ADOLESCENT; ADULT; ANIMALS; ANTI-ANXIETY AGENTS; ANXIETY; DISEASE MODELS, ANIMAL; DOSE-RESPONSE RELATIONSHIP, DRUG; GABA-A RECEPTOR AGONISTS; HETEROCYCLIC COMPOUNDS WITH 4 OR MORE RINGS; HUMANS; HYDROCARBONS, FLUORINATED; MALE; MICE; MIDDLE AGED; PROTEIN SUBUNITS; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, GABA-A; SAIMIRI; SPECIES SPECIFICITY; TIME FACTORS; YOUNG ADULT;

EID: 79952132527     PISSN: 02698811     EISSN: 14617285     Source Type: Journal    
DOI: 10.1177/0269881109354928     Document Type: Article

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