SKF 89976A is a GABA transporter type 1 inhibitor with IC50 of 0.13, 550, 944 and 7210 μM for hGABA T-1, rGABa T-2, hGABA T-3 and hBGT-1 respectively. SKF-89976A is selective for GABA T-1. This compound inhibits transport current competitively (Ki = 7 μM) and transmitter-gated current non-competitively.