AWD 131-138

AWD 131-138 is a new low-affinity partial benzodiazepine receptor agonist, which has potent anticonvulsant and anxiolytic properties in rodent models. AWD 131-138 dose-dependently stimulated GABA currents (Recombinant gamma aminobutyric acid A (GABA(A)) receptors of the subunit compositions alpha1beta2gamma2, alpha1beta3gamma2, alpha2beta2gamma2, alpha3beta2gamma2 and alpha5beta2gamma2). At 10 microM AWD 131-138, this allosteric stimulation amounted to nearly 12-21% of the maximal stimulation achieved using diazepam in average. AWD 131-138 did not produce midazolam-like responding or alter response rates at cumulative doses up to 18.0 mg/kg i.m. (plasma levels over 2100 ng/ml).