Rufinamide-¹⁵N-d₂

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.¹ It inhibits the activation of voltage-gated sodium channel 1.1 (Na_v1.1) when used at a concentration of 100 µM.² Rufinamide inhibits Na_v1.1, but not Na_v1.2, Na_v1.3, and Na_v1.6, opening and increases the action potential threshold in primary rat hippocampal neurons. It is an inhibitor of carbonic anhydrase VA (CAVA; K_i = 343.8 nM) that is selective for CAVA over CAI and CAII (K_is = >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 (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.^5,6 Formulations containing rufinamide have been used in the treatment of seizures associated with Lennox-Gastaut Syndrome (LGS).

WARNING This product is not for human or veterinary use.

1. Wheless, J.W., and Vazquez, B. Rufinamide: A novel broad-spectrum antiepileptic drug. Epilepsy Curr. 10(1), 1-6 (2010).

2. Gilchrist, J.J., Dutton, S., Diaz-Bustamante, M., et al. Na_v1.1 modulation by a novel triazole compound attenuates epileptic seizures in rodents. ACS 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 inhibitors. Eur. J. Med. Chem. 181, 111565 (2019).

4. Gáll, Z., Orbán-Kis, K., and Szilágyi, T. Differential effects of sodium channel blockers on in vitro induced epileptiform activities. Arch. 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 models. Epilepsia 49(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 hippocampus. Arch. Pharm. Res. 41(7), 776-783 (2018).