Retigabine是一种抗惊厥化合物，可激活低阈值电压门控钾通道。
Cas No.:150812-12-7
Sample solution is provided at 25 µL, 10mM.
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Retigabine is an anticonvulsant compound that activates low-threshold voltage-gated potassium channels [1]. Retigabine enhances potassium currents via destabilization of a closed conformation or stabilization of the open conformation of the potassium Kv7.2-7.3 channels[2]. Retigabine has been widely used to stabilize the resting membrane potential, reduce brain excitability, and enhance the current mediated by gamma-aminobutyric acid (GABA)[3].
In vitro, Retigabine treatment (10µM) for 48 hours prevented L-glutamate toxicity in PC12 cells, restored cell viability, and reduced the generation of reactive oxygen intermediates [4].
In vivo, Retigabine treatment via intraperitoneal injection at a dose of 15mg/kg every four hours for 12 hours significantly promoted the apoptosis of brain neurons in newborn rats[5].
References:
[1] Splinter M Y. Ezogabine (retigabine) and its role in the treatment of partial-onset seizures: a review[J]. Clinical therapeutics, 2012, 34(9): 1845-1856. e1.
[2] Czuczwar P, Wojtak A, Cioczek-Czuczwar A, et al. Retigabine: the newer potential antiepileptic drug[J]. Pharmacological Reports, 2010, 62(2): 211-219.
[3] Stafstrom C E, Grippon S, Kirkpatrick P. Ezogabine (retigabine)[J]. Nature Reviews Drug Discovery, 2011, 10(10): 729-730.
[4] Seyfried J, Evert B O, Rundfeldt C, et al. Flupirtine and retigabine prevent L-glutamate toxicity in rat pheochromocytoma PC 12 cells[J]. European journal of pharmacology, 2000, 400(2-3): 155-166.
[5] Brown L, Gutherz S, Kulick C, et al. Profile of retigabine‐induced neuronal apoptosis in the developing rat brain[J]. Epilepsia, 2016, 57(4): 660-670.
Retigabine是一种抗惊厥化合物，可激活低阈值电压门控钾通道[1]。Retigabine通过使钾通道Kv7.2-7.3的闭合态失稳或开放态稳定来增强钾电流[2]。Retigabine已被广泛用于稳定静息膜电位、降低脑兴奋性，并增强γ-氨基丁酸介导的电流[3]。
在体外，10µM的Retigabine处理PC12细胞48小时，可防止L-谷氨酸的细胞毒性，恢复细胞活力，并减少活性氧中间产物的生成[4]。
在体内，每四小时腹腔注射15mg/kg剂量的Retigabine，持续12小时，显著促进了新生大鼠脑神经元的凋亡[5]。
| Cell experiment [1]: | |
Cell lines | PC12 cells |
Preparation Method | PC12 cells were maintained in Dulbecco's modified Eagle medium (DMEM) supplemented with 5% fetal calf serum, 10% horse serum, and 50μg/ml penicillin/streptomycin in a humidified atmosphere containing 5% CO2. Cells were seeded in 96-well plates at a density of 1×105 cells and cultured overnight. After 48h of treatment with l-glutamate (10mM) and 10µM of Retigabine, the cell viability was measured. |
Reaction Conditions | 10µM; 48h |
Applications | Retigabine treatment significantly enhanced the viability of PC12 cells exposed to l-glutamate. |
| Animal experiment [2]: | |
Animal models | Sprague-Dawley rat pups |
Preparation Method | Sprague-Dawley rat pups (7 days old) were maintained in a temperature-controlled (21°C) room with a 12h light cycle. The mice in the treatment group were given an intraperitoneal injection of a 15mg/kg dose of Retigabine every four hours for a total of 12 hours. Control groups received equivalent volumes of saline vehicle (0.01ml/g body weight). Pups were perfused transcardially with ice-cold phosphate buffer, followed by 4% paraformaldehyde and brains were collected for analysis. |
Dosage form | 15mg/kg; every 4 hours for 12 hours; i.p. |
Applications | Retigabine treatment promoted the apoptosis of brain neurons in newborn rats. |
References: | |
| Cas No. | 150812-12-7 | SDF | |
| 别名 | 瑞替加滨 | ||
| 化学名 | (E)-ethyl hydrogen (2-amino-4-((4-fluorobenzyl)amino)phenyl)carbonimidate | ||
| Canonical SMILES | CCO/C(O)=N/C1=C(N)C=C(NCC2=CC=C(F)C=C2)C=C1 | ||
| 分子式 | C16H18FN3O2 | 分子量 | 303.33 |
| 溶解度 | ≥ 12.95mg/mL in DMSO | 储存条件 | Store at -20°C |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.2967 mL | 16.4837 mL | 32.9674 mL |
| 5 mM | 659.3 μL | 3.2967 mL | 6.5935 mL |
| 10 mM | 329.7 μL | 1.6484 mL | 3.2967 mL |
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- Purity: >98.00% Appearance: A solid
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