Abstract
GABA, the principal inhibitory neurotransmitter in the cerebral cortex, maintains the inhibitory tone that counterbalances neuronal excitation. The identification and subsequent development of GABA-transport inhibitors has shown the important role that GABA transporters play in the control of the CNS. To date, four GABA transporters have been cloned (GAT1–4). Compounds that inhibit GABA uptake are targets for epilepsy treatment. Currently, they are also being investigated for other possible indications such as the treatment of psychosis, general anxiety and sleep disorders, drug addiction, acute and chronic pain. These and other issues are discussed in this article.
Financial & competing interests disclosure
The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.
No writing assistance was utilized in the production of this manuscript.