Gamma-aminobutyric acid (GABA) is the primary inhibitory neurotransmitter in the central nervous system, causing a hyperpolarization of the membrane through the opening of a chloride channel associated with the GABAA receptor (GABAA-R) subtype. GABA plasma membrane transporters (GATs) influence synaptic neurotransmission by high-affinity uptake and release of GABA. To date, four distinct GABA transporters have been identified: GAT-1, GAT-2, GAT-3, and BGT-1. GAT-1, the most abundant of the transporters, is found predominantly in neurons, but also in some specialized glia. GAT-1 is thought to play a key role in epileptogenesis.