Biochem/physiol Actions
Reversible: no
Primary TargetGABA Transaminase
General description
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)
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Other Notes
Abbot, E.L., et al. 2006. Br. J. Pharmacol.147, 298.Schmid, L., et al. 1996. J. Pharmacol. Exp. Therap.276, 977.
Packaging
10 mg in Glass bottle
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Warning
Toxicity: Standard Handling (A)
This product has met the following criteria: