Current Medicinal Chemistry

Atta-ur-Rahman, FRS
Honorary Life Fellow
Kings College
University of Cambridge


Translate in Chinese

GABA System as a Target for New Drugs

Author(s): P. Kowalczyk and K. Kulig

Affiliation: Department of Physicochemical Drug Analysis, Department of Pharmaceutical Chemistry, Jagiellonian University Medical College, Medyczna 9, 30-688 Krakow, Poland.


4-Aminobutyric acid is an inhibitory neurotransmitter involved in the control of neuronal activity in the mammalian central nervous system. There is considerable direct and indirect evidence that impaired activity of GABAmediated inhibitory synapses may be an important causative factor in experimental and clinical seizure disorders. This review is focused on the recent development of compounds which can influence GABA neurotransmission by affecting the GABA receptors, the plasma-membrane GABA transporters (GATs) and catabolic enzyme GABA-transaminase (GABAT). These compounds have been primarily investigated in relation to epilepsy, but it has also been found that a decrease in GABA neurotransmission appears to be involved in the aetiology of several neurological disorders such as insomnia, spasticity, neuropathic pain, anxiety and other mental disorders.

Keywords: GABA, GABA uptake inhibitors, GABAA receptor ligands, GABAB receptor ligands, GABAC receptor ligands, GABA aminotransferaseinhibitors.

Order Reprints Order Eprints Rights & PermissionsPrintExport

Article Details

Page: [3294 - 3309]
Pages: 16
DOI: 10.2174/0929867321666140601202158