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.
GABA, GABA uptake inhibitors, GABAA receptor ligands, GABAB receptor ligands, GABAC receptor ligands,
Department of Physicochemical Drug Analysis, Department of Pharmaceutical Chemistry, Jagiellonian University Medical College, Medyczna 9, 30-688 Krakow, Poland.