In Vivo Characterization and Dynamic Receptor Occupancy Imaging of TPA023B, an α2/α3/α5 Subtype Selective γ-Aminobutyric Acid-A Partial Agonist

Biological Psychiatry

Volumn 64, Issue 2, 2008, Pages 153-161

  Van Laere, Koen ^a   Bormans, Guy ^a   Sanabria Bohórquez, Sandra M ^c   de Groot, Tjibbe ^a   Dupont, Patrick ^a   De Lepeleire, Inge ^c   de Hoon, Jan ^b   Mortelmans, Luc ^a   Hargreaves, Richard J ^c   Atack, John R ^d,e   Burns, H Donald ^c  

^a UNIVERSITY OF LEUVEN   (Belgium)

^b UNIVERSITY HOSPITALS LEUVEN   (Belgium)

^c MERCK RESEARCH LABORATORIES   (United States)

^d NEUROSCIENCE RESEARCH CENTRE   (United Kingdom)

^e JOHNSON AND JOHNSON PHARMACEUTICAL RESEARCH AND DEVELOPMENT   (United States)

Author keywords

Anxioselectivity; flumazenil; GABA A receptor subtypes; occupancy; positron emission tomography

Indexed keywords

2',6 DIFLUORO 5' [3 (1 HYDROXY 1 METHYLETHYL)IMIDAZO[1,2 B][1,2,4]TRIAZIN 7 YL][1,1' BIPHENYL] 2 CARBONITRILE; 4 AMINOBUTYRIC ACID RECEPTOR STIMULATING AGENT; FLUMAZENIL C 11; GAMMA AMINOBUTYRIC ACID A ALPHA2 PARTIAL AGONIST; GAMMA AMINOBUTYRIC ACID A ALPHA3 PARTIAL AGONIST; GAMMA AMINOBUTYRIC ACID A ALPHA5 PARTIAL AGONIST; GAMMA AMINOBUTYRIC ACID A PARTIAL AGONIST; PLACEBO; TPA 023B; TRACER;

ADULT; ARTICLE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; DOUBLE BLIND PROCEDURE; DRUG BINDING SITE; HUMAN; IN VIVO STUDY; MALE; NORMAL HUMAN; PHASE 1 CLINICAL TRIAL; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; RANDOMIZATION; RANDOMIZED CONTROLLED TRIAL; RECEPTOR BINDING; RECEPTOR OCCUPANCY; SINGLE DRUG DOSE;

ADMINISTRATION, ORAL; ADULT; BIOLOGICAL AVAILABILITY; BRAIN; CARBON RADIOISOTOPES; DOUBLE-BLIND METHOD; FLUMAZENIL; GABA AGONISTS; HUMANS; KINETICS; MALE; POSITRON-EMISSION TOMOGRAPHY; PYRIDAZINES; RECEPTORS, GABA-A; TRIAZOLES;

EID: 45449099066     PISSN: 00063223     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.biopsych.2008.01.021     Document Type: Article

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