γ-aminobutiric acid (GABA) is the major inhibitory neurotransmitter in the mammalian central nervous system. Transmission via GABA can be halted by its reuptake through GABA transporters (GATs). These membrane proteins belong to the super family of slc6 genes which encode transporters responsible for the uptake of dopamine, serotonin, norepinephrine, glycine and GABA in a Na+-dependent manner. To date, four GATs have been identified: GAT-1, GAT-2, GAT-3 and BGT-1. GATs couple the transport of one GABA molecule to 2 Na+ ions and one Cl– ion.