A sodium channel blocker (IC50 = 138 nM in a radioligand binding assay); inhibits sodium uptake in a dose-dependent manner in rat cortical synaptosomes; protective against MES-induced seizures in mice (ED50s = 4.7 and 6.3 mg/kg

Eslicarbazepine Acetate – 5 mg

Brand:
Cayman
CAS:
236395-14-5
Storage:
-20
UN-No:
Non-Hazardous - /

Eslicarbazepine acetate is a sodium channel blocker (IC50 = 138 nM in a radioligand binding assay).{40363} 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.{40364} 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.{40365}  

 

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Description

A sodium channel blocker (IC50 = 138 nM in a radioligand binding assay); inhibits sodium uptake in a dose-dependent manner in rat cortical synaptosomes; protective against MES-induced seizures in mice (ED50s = 4.7 and 6.3 mg/kg, for oral and i.p. administration respectively); high-dose administration (30 mg/kg) prevents picrotoxin-induced seizures; low-dose administration (10 mg/kg) reduces seizure number and duration

Formal name: (10S)-10-(acetyloxy)-10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide

Synonyms:  BIA 2-093

Molecular weight: 296.3

CAS: 236395-14-5

Purity: ≥95%

Formulation: A solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Research Area|Neuroscience|Seizure Disorders

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