化学信息：
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化学名
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ethyl N-[2-amino-4-[(4-fluorophenyl)methylamino]phenyl]carbamate
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简称
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Retigabine
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别名
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D-23129, Ezogabine, D23129, D 23129
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中文名
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瑞替加滨
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化学式
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C16H18FN3O2
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分子量
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303.33
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CAS号
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150812-12-7
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纯度
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98%
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溶剂/溶解度
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Water<1mg/ml; DMSO4mg/ml; Ethanol<1mg/ml
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溶液配制
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5mg加入1.65ml DMSO，或者每3.03mg加入1ml DMSO，配制成10mM溶液。SF8993-10mM用DMSO配制。
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生物信息：
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产品描述
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Retigabine (Ezogabine; D23129) is a Kv7.2-7.5 (KCNQ2-5) neuronal potassium channel opener witrh anticonvulsant activity.
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信号通路
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Transmembrane Transporters
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靶点
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Kv7.2-7.5
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－
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－
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－
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－
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IC50
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－
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－
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－
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－
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－
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体外研究
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Retigabine (D-23129) is a novel antiepileptic compound with broad spectrum and potent anticonvulsant properties, both in vitro and in vivo. The compound was shown to activate a K+ current in neuronal cells. The pharmacology of the induced current displays concordance with the published pharmacology of the M-channel, which recently was correlated to the KCNQ2/3 K+ channel heteromultimere. Retigabine is a novel anticonvulsant with an unknown mechanism of action. Application of 10μM retigabine to oocytes expressing the KCNQ2/3 heteromeric channel shifted both the activation threshold and voltage for half-activation by approximately 20mV in the hyperpolarizing direction, leading to an increase in current amplitude at test potentials between 80mV and +20mV. Retigabine also had a marked effect on KCNQ current kinetics, increasing the rate of channel activation but slowing deactivation at a given test potential. Retigabine shifted the voltage dependence of channel activation with an EC50value of 1.6±0.3μM (slope factor was 1.2±0.1, n=4 to 5 cells per concentration). Retigabine (0.1 to 10μM) also slowed the rate of channel deactivation, predominantly by increasing the contribution of a slowly deactivating tail current component. Administration of centrally acting M-channel opener retigabine (2.5 and 7.5mg/kg) can dose-dependently raise the head withdrawal threshold of mechanical allodynia, and this analgesic effect can be reversed by the specific KCNQ channel blocker XE991 (3mg/kg). Food intake was increased significantly by the administration of retigabine (2.5 and 7.5mg/kg), and this effect was reversed by XE991 (3mg/kg). Furthermore, intracerebralventricular injection of retigabine further confirmed the analgesic effect of central retigabine on inflammatory TMJ. Retigabine exerted both antiepileptogenic and antiictogenic effects under conditions of rapid kindling model.
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体内研究
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N/A
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临床实验
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N/A
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特征
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N/A
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相关实验数据(此数据来自于公开文献，碧云天并不保证其有效性)：
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酶活性检测实验
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方法
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N/A
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细胞实验
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细胞系
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N/A
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浓度
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N/A
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处理时间
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N/A
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方法
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N/A
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动物实验
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动物模型
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N/A
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配制
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N/A
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剂量
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N/A
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给药方式
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N/A
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参考文献：
1. M.J. Brodie, H. Lerche,, A. Gil-Nagel, et al. Neurology. 2010 November 16, 75(20), 1817-1824 .
2. S Y M Yeung, M Schwake, et al. Br J Pharmacol. 2008 September, 155(1), 62-72.
3. Geraldine M Ferron, Alain Patat, Virginia Parks, et al. Br J Clin Pharmacol. 2003 July, 56(1), 39-45.
包装清单：
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产品编号
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产品名称
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包装
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SF8993-10mM
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Retigabine (Potassium Channel开放剂)
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10mM×0.2ml
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SF8993-5mg
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Retigabine (Potassium Channel开放剂)
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5mg
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SF8993-25mg
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Retigabine (Potassium Channel开放剂)
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25mg
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—
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说明书
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1份
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保存条件：
-20℃保存，至少一年有效。5mg和25mg包装也可室温保存，至少6个月有效。如果溶于非DMSO溶剂，建议分装后-80℃保存，预计6个月内有效。
注意事项：
本产品对人体有毒，操作时请特别小心，并注意有效防护以避免直接接触人体或吸入体内。
本产品仅限于专业人员的科学研究用，不得用于临床诊断或治疗，不得用于食品或药品，不得存放于普通住宅内。
为了您的安全和健康，请穿实验服并戴一次性手套操作。
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