Male CD1 mice were deprived of food for at least 2 h before oral administration of CGS-9895 (0.1, 0.3, 1, 3, 10, 30, 100 mg/kg). 1 h after drug treatment, mice were challenged with 60 mg/kg i.v. pentylenetetrazole. No antipentylenetetrazole activity of CGS 9895 could be detected at doses from 1-100 mg/kg.

The membranes from rat forebrains were prepared and washed. [35S]TBPS binding responses to varying concentrations of diazepam were measured in the presence or absence of 800 nM diazepam. Varying concentrations of CGS 9895 were coincubated with either the solvent or 800 nM diazepam. CGS 9895 increased [35S]TBPS binding in a concentration-dependent manner