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Rufinamide-15N-d2 is intended for use as an internal standard for the quantification of rufinamide by GC- or LC-MS. Rufinamide is an anticonvulsant.1 It inhibits the activation of voltage-gated sodium channel 1.1 (Nav1.1) when used at a concentration of 100 μM.2 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).3 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.4 It inhibits seizures induced by pentylenetetrazole 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.5,6 Formulations containing rufinamide have been used in the treatment of seizures associated with Lennox-Gastaut Syndrome (LGS).

1.Wheless, J.W., and Vazquez, B.Rufinamide: A novel broad-spectrum antiepileptic drugEpilepsy Curr.10(1)1-6(2010) 2.Gilchrist, J.J., Dutton, S., Diaz-Bustamante, M., et al.Nav1.1 modulation by a novel triazole compound attenuates epileptic seizures in rodentsACS Chem. Biol.9(5)1204-1212(2014) 3.Costa, G., Carta, F., Ambrosio, F.A., et al.A computer-assisted discovery of novel potential anti-obesity compounds as selective carbonic anhydrase VA inhibitorsEur. J. Med. Chem.181111565(2019) 4.Gáll, Z., Orbán-Kis, K., and Szilágyi, T.Differential effects of sodium channel blockers on in vitro induced epileptiform activitiesArch. Pharm. Res.40(1)112-121(2017) 5.White, H.S., Franklin, M.R., Kupferberg, H.J., et al.The anticonvulsant profile of rufinamide (CGP 33101) in rodent seizure modelsEpilepsia49(7)1213-1220(2008) 6.Park, J.-A., and Lee, C.-H.Effect of Rufinamide on the kainic acid-induced excitotoxic neuronal death in the mouse hippocampusArch. Pharm. Res.41(7)776-783(2018)

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