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Inhibitor of GABA transaminase
Vigabatrin is an irreversible GABA transaminase (GABA-T) inhibitor.1 It inhibits rat brain GABA-T when used at a concentration of 0.1 mM. Vigabatrin is selective for rat brain GABA-T over P. fluorescens GABA-T at 10 mM and is 100-fold selective over rat brain glutamic acid decarboxylase (GAD). Vigabatrin (1,500 mg/kg) decreases brain GABA-T activity without affecting GAD activity in mice.2 It reduces the incidence of myoclonus in a mouse model of audiogenic seizures.3 Vigabatrin also increases the electroconvulsive threshold in mouse model of maximal electroshock-induced seizures and reduces the number of clonic convulsions induced by pentylenetetrazol in mice.4 Formulations containing vigabatrin have been used in the treatment of seizures and infantile spasms.
1.Lippert, B., Metcalf, B.W., Jung, M.J., et al.4-Amino-hex-5-enoic acid, a selective catalytic inhibitor of 4-aminobutyric-acid aminotransferase in mammalian brainEur. J. Biochem.74(3)441-445(1977) 2.Jung, M.J., Lippert, B., Metcalf, B.W., et al.g-Vinyl GABA (4-amino-hex-5-enoic acid), A new selective irreversible inhibitor of GABA-T: Effects on brain GABA metabolism in miceJ. Neurochem.29(5)797-802(1977) 3.Meldrum, B.S., and Murugaiah, K.Anticonvulsant action in mice with sound-induced seizures of the optical isomers of g-vinyl GABAEur. J. Pharm.89(1-2)149-152(1983) 4.Luszczki, J.J., and Czuczwar, S.J.Isobolographic characterization of interactions between vigabatrin and tiagabine in two experimental models of epilepsyProg. Neuropsychopharmacol. Biol. Psychiatry31(2)529-538(2007)
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