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Retigabine
本半岛bd体育手机客户端 不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Retigabine图片
CAS NO:150812-12-7
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议
100mg电议

半岛bd体育手机客户端 介绍

化学性质

Physical AppearanceA solid
StorageStore at -20°C
M.Wt303.33
Cas No.150812-12-7
FormulaC16H18FN3O2
Solubilityinsoluble in H2O; ≥11.1 mg/mL in EtOH with ultrasonic; ≥12.95 mg/mL in DMSO
Chemical Name(E)-ethyl hydrogen (2-amino-4-((4-fluorobenzyl)amino)phenyl)carbonimidate
Canonical SMILESCCO/C(O)=N/C1=C(N)C=C(NCC2=CC=C(F)C=C2)C=C1
运输条件蓝冰运输或根据您的需求运输。
一般建议为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次半岛bd体育手机客户端 溶解度各有差异，仅做参考。若实验所需浓度过大至半岛bd体育手机客户端 溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

Retigabine is a positive allosteric modulator of KCNQ2-5 (KV7.2-7.5) ion channels, with EC50 values being 1.4, 1.6 and 5.2 μM for KCNQ3/5, KCNQ2/3 and KCNQ4, respectively. Retigabine is the first neuronal potassium channel opener used for the treatment of epilepsy. KCNQ2-5 channels, predominantly expressed in neurons, are important determinants of cellular excitability. The occurrence of human genetic mutations in KCNQ2/3 channels are associated with the syndrome of benign familial neonatal convulsions.

References:

1. Gunthorpe MJ, Large CH, Sankar R. The mechanism of action of retigabine (ezogabine), a first-in-class K+channel opener for the treatment of epilepsy. Epilepsia, 2012, 53(3): 412-424.

2. Stas JI, Bocksteins E, Jensen CS, et al. The anticonvulsant retigabine suppresses neuronal KV2-mediated currents. Scientific Reports, 2016, 6: 35080.

3. De Sarro G, Di Paola ED, Conte G, et al. Influence of retigabine on the anticonvulsant activity of some antiepileptic drugs against audiogenic seizures in DBA/2 mice. Naunyn-Schmiedeberg's Archives of Pharmacology, 2001, 363(3): 330-336.

试验操作

Cell experiment:[2]

Cell lines

HEK293 cells transfected with KV2.1

Reaction Conditions

0.1, 0.3, 1 or 3 μM retigabine for 4 h incubation

Applications

Retigabine reduced the KV2.1 current density in a concentration-dependent manner. The current density was significantly reduced by approximately 2.5-fold after exposure to 1 and 3 μM retigabine. Thus, KV2.1 was identified as a new molecular target for retigabine, with the potential to further explain retigabine's neuroprotective properties.

Animal experiment:[3]

Animal models

DBA/2 mice

Dosage form

0.5 ~ 20 mg/kg

Intraperitoneal administration

Applications

Retigabine exhibited an additive effect when administered in combination with classical anticonvulsants, most notably diazepam, phenobarbital, phenytoin as well as valproate.

Note

The technical data provided above is for reference only.

References:

1. Gunthorpe MJ, Large CH, Sankar R. The mechanism of action of retigabine (ezogabine), a first-in-class K+ channel opener for the treatment of epilepsy. Epilepsia, 2012, 53(3): 412-424.

2. Stas JI, Bocksteins E, Jensen CS, et al. The anticonvulsant retigabine suppresses neuronal KV2-mediated currents. Scientific Reports, 2016, 6: 35080.

3. De Sarro G, Di Paola ED, Conte G, et al. Influence of retigabine on the anticonvulsant activity of some antiepileptic drugs against audiogenic seizures in DBA/2 mice. Naunyn-Schmiedeberg's Archives of Pharmacology, 2001, 363(3): 330-336.

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