|10-羟基-10,11-二氢-5H-二苯并[b,f]氮杂卓-5-甲酰胺|CsnPharm

CAS No.: 29331-92-8

10,11-二氢-10-羟基卡马西平 Catalog No. CSN25458

Synonyms: BIA 2-005;GP 47779;LIC-477

Licarbazepine, also known as BIA-2-005; GP-47779; LIC-477; LIC-477D; TRI-477, is a voltage-gated sodium channel blocker with anticonvulsant and mood-stabilizing effects that is related to oxcarbazepine. It is an active metabolite of oxcarbazepine. In addition, an isomer of licarbazepine, eslicarbazepine ((S)-(+)-licarbazepine), is an active metabolite of eslicarbazepine acetate. Oxcarbazepine and eslicarbazepine acetate are inactive on their own, and behave instead as prodrugs to licarbazepine and eslicarbazepine, respectively, to produce their therapeutic effects.

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描述Licarbazepine, also known as BIA-2-005; GP-47779; LIC-477; LIC-477D; TRI-477, is a voltage-gated sodium channel blocker with anticonvulsant and mood-stabilizing effects that is related to oxcarbazepine. It is an active metabolite of oxcarbazepine. In addition, an isomer of licarbazepine, eslicarbazepine ((S)-(+)-licarbazepine), is an active metabolite of eslicarbazepine acetate. Oxcarbazepine and eslicarbazepine acetate are inactive on their own, and behave instead as prodrugs to licarbazepine and eslicarbazepine, respectively, to produce their therapeutic effects. Licarbazepine is a voltage-gated sodium channel blocker with anticonvulsant and mood-stabilizing effects. OXC (20 mg/kg), (S)-licarbazepine (20 mg/kg), and (R)-licarbazepine (20 mg/kg) all significantly increased the number of SWDs (spike-and-wave discharges), while their duration was unaffected^[1]. S-Lic (S-licarbazepine) is the main enantiomer responsible for anticonvulsant activity and this is proposed to be through the blockade of voltage-gated Na+ channels (VGSCs). ESL (Eslicarbazepine acetate) and S-Lic both have a voltage-dependent inhibitory effect on the Na+ current in N1E-115 neuroblastoma cells expressing neuronal VGSC subtypes including Nav1.1, Nav1.2, Nav1.3, Nav1.6, and Nav1.7^[2]. It is not necessary to routinely determine licarbazepine levels. In specific cases, licarbazepine levels can be useful to assess adherence to treatment and for personalized dose adjustment^[3]. Licarbazepine is well tolerated and has predictable pharmacokinetics^[4].

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.9326 mL
- 19.6631 mL
- 39.3261 mL
- 5 mM
- 0.7865 mL
- 3.9326 mL
- 7.8652 mL
- 10 mM
- 0.3933 mL
- 1.9663 mL
- 3.9326 mL

技术信息

CAS号	29331-92-8	储存条件	粉末 Inert atmosphere,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C15H14N2O2	运输	蓝冰
分子量	254.28	别名	BIA 2-005;GP 47779;LIC-477;LIC-477D;TRI-477;10,11-dihydro-10-hydroxy Carbamazepine;10,11-dihydro-10-hydroxy CBZ;10,11-hydroxy-10,11 Dihydrocarbamezer

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10,11-二氢-10-羟基卡马西平 Catalog No. CSN25458

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