gat-2

6,7-Dimethylisatin (6,7-dimethyl-1H-indole-2,3-dione) inhibits hGAT3 with IC50 of 108 μM. 6,7-Dimethylisatin also inhibits hBGT1, hGAT2.

BPDBA is an effective, selective, and non-competitive inhibitor of the betaine GABA transporter (BGT-1), displaying inhibitory activity against human BGT-1 and mouse GAT2, with IC50 values of 20 μM and 35 μM, respectively.

SKF89976A is a potent GABA uptake inhibitor, which is selective for GAT-1 (IC50 values are 0.13, 550, 944 and 7210 μM for hGAT-1, rGAT-2, hGAT-3 and hBGT-1 respectively). SKF89976A inhibits transport current competitively (Ki = 7 μM) and transmitter-gated current non-competitively (Ki = 0.03 nM). It is able to pass the blood-brain barrier after systemic administration and is active in vivo.

(S)-SNAP5114 is a selective inhibitor of GABA transport, exhibiting IC50 values of 5 μM for hGAT-3 and 21 μM for rGAT-2, and possesses anticonvulsant properties.

Guvacine can enhance the inhibition of spinal neurones by GABA.

SKF89976A hydrochloride (d,l-SKF89976A hydrochloride) is a selective inhibitor GABA transporter such as GAT-1 (IC50s = 0.28 μM), GAT-2 (IC50s = 137.34 μM) and GAT-3(IC50s = 202.8 μM) in CHO cells.

Guvacine hydrobromide, an alkaloid derived from the Areca catechu nut, serves as a potent inhibitor of GABA (GABA uptakp) uptake. It effectively inhibits rat GABA transporter isoforms GAT-1, GAT-2, and GAT-3, with respective IC50 values of 39 μM, 58 μM, and 378 μM [1].