A selective, irreversible inhibitor of GABA transaminase with antiepileptic properties. Covalently binds to the active site of GABA tansaminase to inactivate it in a dose-dependent manner and increases extracellular GABA levels in the brain. Rapidly absorbed following oral administration and is shown to inhibit [3H]GABA uptake across the apical membrane of Caco-2 cell monolayers in a concentration-dependent manner (IC50 = 2.9 mM)
Toxicity: Standard Handling (A)
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
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Schmid, L., et al. 1996. J. Pharmacol. Exp. Therap.276, 977.
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany