Document Classification

Section Type: BACKGROUND

Text: A novel, high-affinity (. 7 -2. 0 nmol) compound that selectively activates the alpha2, alpha 3, and alpha 5 (but not alpha1) gamma-aminobutyric acid-A (GABA (A)) 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 GABA (A) receptors after a single oral dose.