A pan-CA inhibitor and an anticonvulsant
Sulthiame is a pan-inhibitor of carbonic anhydrases (CA; Kis = 6-1,540 nM for CAI, -II, and IV-XIV) and an anticonvulsant.1 It is selective for these CAs over CAIII (Ki = 630 ?M). Sulthiame (10 ?g/ml) also inhibits voltage-gated sodium currents in isolated guinea pig hippocampal CA1 neurons.2 It reduces epileptiform activity induced by 4-aminopyridine in guinea pig hippocampal slices when used at a concentration of 2.5 mM.3 Sulthiame (100-300 mg/kg, i.p.) induces neuronal cell death in neonatal rats.4 It decreases forelimb clonus duration in a rat model of partial epilepsy induced by amygdaloid kindling when administered at doses ranging from 25 to 200 mg/kg.5 Formulations containing sulthiame have been used in the treatment of epilepsy.
1.De Simone, G., Scozzafava, A., and Supuran, C.T.Which carbonic anhydrases are targeted by the antiepileptic sulfonamides and sulfamates?Chem. Biol. Drug Des.74(3)317-321(2009) 2.Madeja, M., Wolf, C., and Speckmann, E.J.Reduction of voltage-operated sodium currents by the anticonvulsant drug sulthiameBrain Res.900(1)88-94(2001) 3.Leniger, T., Wiemann, M., Bingmann, D., et al.Carbonic anhydrase inhibitor sulthiame reduces intracellular pH and epileptiform activity of hippocampal CA3 neuronsEpilepsia43(5)469-474(2002) 4.Manthey, D., Asimiadou, S., Stefovska, V., et al.Sulthiame but not levetiracetam exerts neurotoxic effect in the developing rat brainExp. Neurol.193(2)497-503(2005) 5.Song, H.K., Hamada, K., Yagi, K., et al.Effects of single and repeated administration of sulthiame on amygdaloid kindled seizures in ratsEpilepsy Res.27(2)81-87(1997)
动态评分
0.0