GABA transporters (Gamma-Aminobutyric acid transporters) belong to the family of neurotransmitters known as sodium symporters, also known as solute carrier 6 (SLC6). These are large family of neurotransmitter which are Na+ concentration dependent. They are found in various regions of the brain in different cell types, such as neurons and astrocytes. These transporters are primarily responsible for the regulation of extracellular GABA concentration during basal and synaptic activity. They are responsible to create a GABA gradient which is determined by the membrane potential, and the concentration of Na+ and Cl−. They are also present on the plasma membrane of neurons and glia which help define their function of regulation of GABA concentration as they act as the receptors that facilitate recycling of GABA in the extracellular space. GABA transporters often are the main sites that are aimed by lot of anticonvulsant drugs in order to avoid seizure disorders such as epilepsy.
|CSN17061||SKF-89976A HCl||85375-15-1||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.|
|CSN25410||Saclofen||125464-42-8||Saclofen is a selective antagonist of GABAB receptors.|
|CSN26368||Guvacine HCl||6027-91-4||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).|
|CSN25768||H-DL-Nip-OH||498-95-3||(±)-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.|
|CSN25767||(S)-SNAP 5114||157604-55-2||(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).|