(S)-SNAP 5114 ia an inhibitor of GABA transport. It shows selectivity for GAT-3 and GAT-2 (IC50 values are 5, 21 and 388 μM for hGAT-3, rGAT-2 and hGAT-1 respectively). 

Cinromide是一种抗惊厥药物，通过抑制上皮中性氨基酸转运蛋白B0AT1，表现出对神经系统的保护作用。

SKF-89976A HCl is a selective GABA transporter (GAT-1) inhibitor with IC50s of 0.28 μM, 137.34 μM and 202.8 μM for GAT-1, GAT-2 and GAT-3 in CHO cells, respectively.

Guvacine hydrochloride是从槟榔中提取的一种生物碱，是GABA转运体的抑制剂，对几种克隆的GABA转运体具有适度的选择性，其IC50值分别为14 μM（人类GAT-1）、39 μM（大鼠GAT-1）、58 μM（大鼠GAT-2）、119 μM（人类GAT-3）、378 μM（大鼠GAT-3）和1870 μM（人类BGT-3）。

(±)-Nipecotic acid is an inhibitor of GABA uptake with IC50 values of 8, 106 and 2370 mM for hGABA T-1, hGABA T-3 and hBGT-1 respectively.

Saclofen is a selective antagonist of GABAB receptors.

NNC 711 is a potent and selective inhibitor of GABA uptake by GAT-1 with IC50 values of 0.04, 1700 and 622 μM for hGAT-1, hGAT-3 and hBGT-1 respectively.