Binding affinity to human GABAA alpha3beta3gamma2 receptor expressed in HEK293 cells assessed as GABA-induced membrane potential change preincubated for 3 mins followed by addition of GABA measured after 3 mins by FLIPR assay
Binding affinity to human GABAA alpha1beta3gamma2 receptor expressed in HEK293 cells assessed as GABA-induced membrane potential change preincubated for 3 mins followed by addition of GABA measured after 3 mins by FLIPR assay
Drug metabolism in Sprague-Dawley rat brain assessed as (E)-8-ethynyl-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,5-a][1,4]diazepine-3-carboxylic acid formation at 10 mg/kg, po measured after 120 mins by LC-MS/MS analysis
Anxiolytic-like activity in Swiss Webster mouse marble burying model of anxiety assessed as suppression of marble burying activity at 30 mg/kg, ip administered 30 mins prior to test relative to vehicle-control
Toxicity in Swiss mouse assessed as change in motor coordination by measuring number of falls from the rotating rod at 10 mg/kg, ip administered 30 mins prior to testing measured for 2 mins by rotarod test relative to control
Toxicity in Swiss mouse assessed as change in motor coordination by measuring number of falls from the rotating rod at 30 mg/kg, ip administered 30 mins prior to testing measured for 2 mins by rotarod test relative to control
Modulation of recombinant GABA alpha2beta3gamma2 receptor (unknown origin) expressed in Xenopus laevis oocytes assessed as change in GABA-induced EC(3 to 6) current at 100 nM by two-electrode voltage clamp assay
Modulation of recombinant GABA alpha3beta3gamma2 receptor (unknown origin) expressed in Xenopus laevis oocytes assessed as change in GABA-induced EC(3 to 6) current at 100 nM by two-electrode voltage clamp assay
Modulation of recombinant GABA alpha1beta3gamma2 receptor (unknown origin) expressed in Xenopus laevis oocytes assessed as change in GABA-induced EC(3 to 6) current at 1 uM by two-electrode voltage clamp assay
Modulation of recombinant GABA alpha2beta3gamma2 receptor (unknown origin) expressed in Xenopus laevis oocytes assessed as change in GABA-induced EC(3 to 6) current at 1 uM by two-electrode voltage clamp assay
Modulation of recombinant GABA alpha3beta3gamma2 receptor (unknown origin) expressed in Xenopus laevis oocytes assessed as change in GABA-induced EC(3 to 6) current at 1 uM by two-electrode voltage clamp assay