Title: In vivo characterization and dynamic receptor occupancy imaging of TPA023B, an alpha 2/alpha 3/alpha 5 subtype selective gamma-aminobutyric acid-A partial agonist
Authors: Van Laere, Koen ×
Bormans, Guy
Sanabria-Bohorquez, Sandra M
de Hoon, Jan
de Groot, Tjibbe
De Lepeleire, Inge
Dupont, Patrick
Mortelmans, Luc
Hargreaves, Richard J
Atack, John R
Burns, H. Donald #
Issue Date: Jul-2008
Publisher: Elsevier
Series Title: Biological Psychiatry vol:64 issue:2 pages:153-161
Abstract: Background: A novel, high-affinity (.7-2.0 nmol) compound that selectively activates the alpha 2, alpha 3, and alpha 5 (but not alpha 1) gamma-aminobutyric acid-A(GABAA) receptor subtypes, TPA023B (2',6-difluoro-5'-[3-(1-hydroxy-1-methylethyl) imidazo[1,2-b][1,2,4]triazin-7-yl][1,1'-biphenyl]-2-carbonitrile) was pharmacologically characterized and studied by means of positron emission tomography (PET) to determine dynamic occupancies of the benzodiazepine binding site of human brain GABAA receptors after a single oral dose.
ISSN: 0006-3223
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Radiopharmacy
Clinical Pharmacology Centre (-)
Nuclear Medicine & Molecular Imaging
Research Group Experimental Neurology
Laboratory for Cognitive Neurology
× corresponding author
# (joint) last author

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