LU-32-176B, a GABA transporter 1 (GAT1) selective inhibitor, is found to exert a synergistic anticonvulsant action with GAT2 transport inhibitor EF1502. LU-32-176B inhibits neurons , astrocytes and mGAT1 with the IC 50 values of 2μM, 1μM, 4μM, respectively.