Eslicarbazepine Acetate

Eslicarbazepine acetate is a sodium channel blocker (IC50 = 138 nM in a radioligand binding assay). It inhibits sodium uptake in a dose-dependent manner in rat cortical synaptosomes at concentrations ranging from 30-300 µM. In vivo, oral and i.p. administration of eslicarbazepine acetate is protective against seizures induced by maximal electroshock (MES) in mice with ED50 values of 4.7 and 6.3 mg/kg, respectively, which are well below the median toxic dose (TD50) values of 358.7 and 78.6 mg/kg for oral and i.p. administration respectively. High-dose administration (30 mg/kg) of eslicarbazepine acetate prevents picrotoxin-induced seizures in rats. Low-dose administration (10 mg/kg) does not suppress picrotoxin-induced seizures, however, it reduces seizure number and duration. Formulations containing eslicarbazepine acetate have been used for the treatment of partial-onset seizures.Formal Name: (10S)-10-(acetyloxy)-10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide. CAS Number: 236395-14-5. Synonyms: BIA 2-093. Molecular Formula: C17H16N2O3. Formula Weight: 296.3. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMF: 20mg/mL, DMSO: 5mg/mL, Ethanol: 10mg/mL. SMILES: O=C(C)O[C@@H]1C2=C(C=CC=C2)N(C(N)=O)C3=C(C=CC=C3)C1. InChi Code: InChI=1S/C17H16N2O3/c1-11(20)22-16-10-12-6-2-4-8-14(12)19(17(18)21)15-9-5-3-7-13(15)16/h2-9,16H,10H2,1H3,(H2,18,21)/t16-/m0/s1. InChi Key: QIALRBLEEWJACW-INIZCTEOSA-N.