236395-14-5 Usage
Description
Different sources of media describe the Description of 236395-14-5 differently. You can refer to the following data:
1. Although epilepsy is a neurological disorder with varying etiology
and severity, the common feature is unprovoked, recurring seizures.
Even when traditional AEDs, such as phenobarbital,
phenytoin, carbamazepine, and valproate, control seizure activity, their
effectiveness is hampered by considerable side effects and the tendency
for drug-drug interactions. Designed for improved efficacy and safety,
eslicarbazepine acetate is a third-generation AED that has been approved
as adjunctive therapy for partial-onset seizures with or without secondary generalization. As a member of the carbamazepine family (first generation), it is the prodrug of eslicarbazepine and the active metabolite of
oxcarbazepine (second generation).
.
2. 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.
Chemical Properties
White to Off-White Solid
Originator
BIAL Group (Spain)
Uses
Different sources of media describe the Uses of 236395-14-5 differently. You can refer to the following data:
1. Eslicarbazepine acetate, (BIA 2-093), is a promising antiepileptic drug structurally related to Carbamazepine and Oxcarbazepine.
2. Eslicarbazepine acetate, (BIA 2-093), is a promising antiepileptic drug structurally related to Carbamazepine and Oxcarbazepine. Neuroprotective & Neuroresearch product.
Definition
ChEBI: The acetate ester, with S configuration, of licarbazepine. An anticonvulsant, it is approved for use in Europe and the United States as an adjunctive therapy for epilepsy.
Brand name
Zebinix; Exalief, Stedesa
Side effects
The most
common adverse events occurring with an incidence of >2% were dizziness, somnolence, nausea, diplopia, headache, vomiting, abnormal coordination, blurred vision, vertigo, and fatigue. While most of these side effects appeared to be mild to moderate, they did display a dose dependency. Although eslicarbazepine acetate is only contraindicated in patients with a known hypersensitivity to the carbamazepine family of AEDs, caution should be exercised in patients with cardiac conduction abnormalities (potential for prolongations in PR intervals), renal impairment, and in patients of Han Chinese and Thai origin since the presence of HLA-B*1502 allele in these individuals has been shown to be strongly associated with the risk of developing Stevens-Johnson syndrome. Regarding drug interactions, eslicarbazepine acetate may decrease the effectiveness of hormonal contraceptives, so alternative or additional methods of contraception should be considered.
Check Digit Verification of cas no
The CAS Registry Mumber 236395-14-5 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 2,3,6,3,9 and 5 respectively; the second part has 2 digits, 1 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 236395-14:
(8*2)+(7*3)+(6*6)+(5*3)+(4*9)+(3*5)+(2*1)+(1*4)=145
145 % 10 = 5
So 236395-14-5 is a valid CAS Registry Number.
InChI:InChI=1/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
236395-14-5Relevant articles and documents
Synthesis method of high-purity stable crystal form of escilitalopine acetate
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Paragraph 0032-0035, (2022/03/18)
The present invention discloses a high-purity method for the synthesis of escitazepine acetate and a novel stable crystal form thereof. The preparation method disclosed in the present invention is achieved by the following steps: 10-methoxyiminopyrene as the starting material, the starting material is dissolved in acetone and deprotected to form 10-carbonyliminocarbenzene; the use of dichloromethane, borane dimethyl sulfide, (R)-2-methyl -CBS- oxazoleboran asymmetrical reduction to generate (10S)-10-hydroxyiminopyrene; (10S)-10-hydroxyiminostilbeneylated into esters, amidated with chlorosulfonyl isocyanate, To obtain escilitalopine acetate and a stable new crystal form. The preparation method provided by the present invention is simple synthesis process, few reaction steps, less pollution, raw materials are readily available and inexpensive, the final product is easy to purify and separate and the crystal form is stable, and the industrial application prospects are broad.
Recrystallization purification process for precursor reactant of asymmetric catalytic hydrogenation reaction
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Paragraph 0027; 0028; 0029; 0032-0038, (2018/12/13)
The invention provides a recrystallization purification device for a precursor reactant prepared from Eslicarbazepine and a derivative thereof. The device is characterized in that a recrystallizationpurification process and a recrystallization purification device are used, unreacted raw materials, byproducts and impurities in the precursor reactant are removed, toxicity of a chiral catalyst is eliminated, the conversion rate of the chiral catalyst is greatly increased, the yield of asymmetric hydrogenation is effectively increased, high production efficiency is achieved, and the cost performance of on-scale production of Eslicarbazepine and the derivative thereof is effectively increased.
Brain-targeting eslicarbazepine ester prodrug and application thereof
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Paragraph 0098, (2017/08/28)
The invention relates to an eslicarbazepine ester prodrug and an application thereof, wherein the prodrug is a compound represented by the formula (I) or optical isomers or physiologically acceptable salts of the compound represented by the formula (I), wherein R represents a lipophilic substituent. The compound represented by the formula (I) is the eslicarbazepine ester prodrug containing the lipophilic substituent, is converted into eslicarbazepine through metabolism in vivo to play pharmacological effects, and can be applied in preparation of drugs for treatment, prevention or adjuvant treatment of central nervous system diseases, such as epilepsy and the like.
