title: GABA transporters as targets for new drugs.
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.
authors.affiliation: Department of Pharmacodynamics, Jagiellonian University, Medical College, Cracow, Poland.
authors.forename: Kinga
authors.initials: K
authors.lastname: Sałat
authors.forename: Katarzyna
authors.initials: K
authors.lastname: Kulig
mesh_terms: D000818:Animals; D001692:Biological Transport / Q000502:physiology; D018756:GABA Antagonists / Q000737:chemistry / Q000378:metabolism; D050485:GABA Plasma Membrane Transport Proteins / Q000737:chemistry / Q000235:genetics / Q000378:metabolism*; D006801:Humans; D015394:Molecular Structure; D004364:Pharmaceutical Preparations / Q000737:chemistry / Q000378:metabolism*; D005680:gamma-Aminobutyric Acid / Q000031:analogs & derivatives / Q000378:metabolism*
chemical_list: D018756:GABA Antagonists; D050485:GABA Plasma Membrane Transport Proteins; D004364:Pharmaceutical Preparations; D005680:gamma-Aminobutyric Acid