GABATransporters

GABA transporters, also known as GATs, are a family of proteins responsible for the reuptake of gamma-aminobutyric acid (GABA) from the synaptic cleft into neurons and glial cells. GABA is the primary inhibitory neurotransmitter in the mammalian central nervous system, and its efficient removal from the synapse is crucial for regulating neuronal excitability and preventing excessive inhibition.

There are four known subtypes of GABA transporters: GAT1, GAT2, GAT3, and BGT1. Each subtype exhibits distinct tissue distribution, substrate affinity, and regulatory mechanisms. GAT1 is the most widely expressed subtype and plays a major role in GABAergic neurotransmission by clearing GABA from the synaptic cleft. GAT2 is primarily found in the liver and kidneys, though it also plays a role in GABAergic signaling in the brain. GAT3 is localized to astrocytes and is thought to contribute to the uptake of GABA from the extracellular space. BGT1, also known as betaine transporter 1, is primarily involved in betaine transport but can also transport GABA.

The function of GABA transporters is critical for maintaining the delicate balance of excitation and inhibition in the brain. Dysregulation of GABA transporter activity has been implicated in various neurological and psychiatric disorders, including epilepsy, anxiety disorders, and schizophrenia. Therefore, GABA transporters represent important therapeutic targets for the development of drugs aimed at modulating GABAergic neurotransmission. For example, inhibitors of GAT1 have been investigated for their potential anticonvulsant effects.