Novel, highly potent and in vivo active inhibitor of GABA transporter subtype 1 with anticonvulsant, anxiolytic, antidepressant and antinociceptive properties
文摘
DDPM-2571, a guvacine analogue, is a novel, potent inhibitor of GABA transporter GAT1. It has prominent anticonvulsant properties in chemically-induced seizures in mice. It demonstrates anxiolytic-like and antidepressant-like properties in vivo. DDPM-2571 has antinociceptive activity in acute and tonic pain models in mice. These pharmacological activities are observed at doses lower than those of tiagabine.