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In pharmacology, a GABA transaminase inhibitor is an enzyme inhibitor that acts upon GABA transaminase. Inhibition of GABA transaminase enzymes reduces the degradation of GABA, leading to increased neuronal GABA concentrations.

Examples include valproic acid, vigabatrin, phenylethylidenehydrazine (and drugs that metabolize to it, such as phenelzine), ethanolamine-O-sulfate (EOS), and L-cycloserine.

Certain members of this class are used as anticonvulsants.

References

1. Ciesielski, L.; Simler, S.; Gensburger, C.; Mandel, P.; Taillandier, G.; Benoit-Guyod, J. L.; Boucherle, A.; Cohen-Addad, C.; Lajzerowicz, J. (1979). "GABA Transaminase Inhibitors". GABA—Biochemistry and CNS Functions. Advances in Experimental Medicine and Biology. Vol. 123. pp. 21–41. doi:10.1007/978-1-4899-5199-1_2. ISBN 978-1-4899-5201-1. PMID 390993.
2. Bruni, J.; Wilder, B. J. (1979). "Valproic acid. Review of a new antiepileptic drug". Archives of Neurology. 36 (7): 393–398. doi:10.1001/archneur.1979.00500430023002. PMID 110294.
3. Wang QP, Jammoul F, Duboc A, et al. (April 2008). "Treatment of epilepsy: the GABA-transaminase inhibitor, vigabatrin, induces neuronal plasticity in the mouse retina". Eur. J. Neurosci. 27 (8): 2177–87. doi:10.1111/j.1460-9568.2008.06175.x. PMC 2933832. PMID 18412635.
4. Gibson, J. P.; Yarrington, J. T.; Loudy, D. E.; Gerbig, C. G.; Hurst, G. H.; Newberne, J. W. (1990). "Chronic toxicity studies with vigabatrin, a GABA-transaminase inhibitor". Toxicologic Pathology. 18 (2): 225–238. doi:10.1177/019262339001800201. PMID 2399411.
5. McKenna, K. F.; McManus, D. J.; Baker, G. B.; Coutts, R. T. (1994). "Chronic administration of the antidepressant phenelzine and its N-acetyl analogue: effects on GABAergic function". Journal of Neural Transmission. Supplementum. 41: 115–122. doi:10.1007/978-3-7091-9324-2_15. ISBN 978-3-211-82521-1. ISSN 0303-6995. PMID 7931216.
6. Polc, P.; Pieri, L.; Bonetti, E. P.; Scherschlicht, R.; Moehler, H.; Kettler, R.; Burkard, W.; Haefely, W. (1986). "L-cycloserine: Behavioural and biochemical effects after single and repeated administration to mice, rats and cats". Neuropharmacology. 25 (4): 411–418. doi:10.1016/0028-3908(86)90236-4. PMID 3012401. S2CID 462885.

• GABA transaminase inhibitors