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, an alkaloid from the nut of Areca catechu, acts as an inhibitor of GABA transporter, and dispalys modest selectivity for cloned GABA transporters with IC50 values of 14 μM (human GAT-1), 39 μM (rat GAT-1), 58 μM (rat GAT-2), 119 μM (human GAT-3), 378 μM (rat GAT-3), and 1870 μM (human BGT-3).

(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). 

(±)-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.