GABA transporters (GAT1, GAT2, GAT3, and BGT1) (GATs/BGT1)

The GABA transporters (GAT1, GAT2, GAT3, and BGT1) are integral membrane proteins belonging to the solute carrier family 6 (SLC6) that mediate the high-affinity uptake of gamma-aminobutyric acid (GABA) from the extracellular space into neurons and glia (UniProt P30531, P48066, P48067, Q9NSD5). GAT1 is the most abundant isoform in the brain, primarily located on presynaptic terminals, and is the primary target for the anticonvulsant drug tiagabine (PubChem CID 60648). GAT3 is predominantly expressed in astrocytes, while GAT2 and BGT1 (Betaine-GABA transporter 1) are found in both the central nervous system and peripheral tissues like the liver and kidney, where BGT1 also functions in osmoregulation (PMID: 23891607). By regulating the duration and intensity of GABAergic signaling, these transporters play a critical role in maintaining the balance between excitation and inhibition in the brain. Dysfunctional GABA transport is linked to several neurological and psychiatric conditions, including epilepsy, schizophrenia, and chronic pain (PMID: 23510511). Therapeutic targeting of these transporters aims to elevate extracellular GABA levels to enhance inhibitory tone, though challenges remain in achieving isoform selectivity to minimize side effects such as sedation and ataxia.

Other names

Sodium- and chloride-dependent GABA transporter 1 (SLC6A1)Sodium- and chloride-dependent GABA transporter 2 (SLC6A13)Sodium- and chloride-dependent GABA transporter 3 (SLC6A11)Sodium- and chloride-dependent betaine-GABA transporter (SLC6A12)Solute carrier family 6 members 1, 11, 12, and 13

Inhibition of GABA reuptake from the synaptic cleft and extracellular space, leading to increased GABAergic tone and enhanced inhibitory neurotransmission (PMID: 23510511).