Rufinamide

Lennox-Gastaut syndrome (LGS) is a severe pediatric epilepsy syndrome characterized by multiple seizure types. Rufinamide is an anticonvulsant. It inhibits the activation of voltage-gated sodium channel 1.1 (Nav1.1) when used at a concentration of 100 µM. 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). 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. It inhibits seizures induced by pentylenetetrazole (Cay-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. Formulations containing rufinamide have been used in the treatment of seizures associated with Lennox-Gastaut Syndrome (LGS).Formal Name: 1-[(2,6-difluorophenyl)methyl]-1H-1,2,3-triazole-4-carboxamide. CAS Number: 106308-44-5. Synonyms: CGP 33101, RUF 331. Molecular Formula: C10H8F2N4O. Formula Weight: 238.2. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 2 mg/ml, DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml, DMSO: 10 mg/ml. SMILES: FC1=CC=CC(F)=C1CN2N=NC(C(N)=O)=C2. InChi Code: InChI=1S/C10H8F2N4O/c11-7-2-1-3-8(12)6(7)4-16-5-9(10(13)17)14-15-16/h1-3,5H,4H2,(H2,13,17). InChi Key: POGQSBRIGCQNEG-UHFFFAOYSA-N.