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)
Biochem/physiol Actions
Primary Target GABA Transaminase
Reversible: no
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Abbot, E.L., et al. 2006. Br. J. Pharmacol.147, 298. Schmid, L., et al. 1996. J. Pharmacol. Exp. Therap.276, 977.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
wgk_germany
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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