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 = 2.9mM).
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