SKF-89976A is a GABA transporters (GATs) type 1 inhibitor.
생물학적 활성
A potent GABA uptake inhibitor, selective for GAT-1 (IC 50 values are 0.13, 550, 944 and 7210 μ M for hGAT-1, rGAT-2, hGAT-3 and hBGT-1 respectively). Inhibits transport current competitively (K i = 7 μ M) and transmitter-gated current non-competitively (K i = 0.03 nM). Able to pass the blood-brain barrier after systemic administration and is active in vivo .