产品描述:
Rufinamide-15N-d2 is intended for use as an internal standard for the quantification of rufinamide (Item No. 18870) by GC- or LC-MS. Rufinamide is an anticonvulsant.{58372} It inhibits the activation of voltage-gated sodium channel 1.1 (Nav1.1) when used at a concentration of 100 µM.{58370} Rufinamide inhibits Nav1.1, but not Nav1.2, Nav1.3, and Nav1.6, opening and increases the action potential threshold in primary rat hippocampal neurons. It is an inhibitor of carbonic anhydrase VA (CAVA; Ki = 343.8 nM) that is selective for CAVA over CAI and CAII (Kis = >10,000 nM for both).{58371} Rufinamide (100 µM) prolongs the preictal phase and reduces seizure-like event frequency in an in vitro model of epileptiform activity in rat hippocampal slices.{58369} It inhibits seizures induced by pentylenetetrazole (Item No. 18682) in a mouse model of epilepsy (ED50 = 54 mg/kg, i.p.) and reduces kainic acid-induced neuronal cell death in the mouse hippocampal CA3 region when used at doses of 25, 50, and 100 mg/kg.{58368,58367} Formulations containing rufinamide have been used in the treatment of seizures associated with Lennox-Gastaut Syndrome (LGS).