Retigabine (Potassium Channel开放剂)

化学名

ethyl N-[2-amino-4-[(4-fluorophenyl)methylamino]phenyl]carbamate

简称

Retigabine

别名

D-23129, Ezogabine, D23129, D 23129

中文名

瑞替加滨

化学式

C₁₆H₁₈FN₃O₂

分子量

303.33

CAS号

150812-12-7

纯度

98%

溶剂/溶解度

Water<1mg/ml; DMSO4mg/ml; Ethanol<1mg/ml

溶液配制

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。

产品描述

Retigabine (Ezogabine; D23129) is a Kv7.2-7.5 (KCNQ2-5) neuronal potassium channel opener witrh anticonvulsant activity.

信号通路

Transmembrane Transporters

靶点

Kv7.2-7.5

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－

－

－

IC50

－

－

－

－

－

体外研究

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.

体内研究

N/A

临床实验

N/A

特征

N/A

酶活性检测实验

方法

N/A

细胞实验

细胞系

N/A

浓度

N/A

处理时间

N/A

方法

N/A

动物实验

动物模型

N/A

配制

N/A

剂量

N/A

给药方式

N/A

产品编号

产品名称

包装

SF8993-10mM

Retigabine (Potassium Channel开放剂)

10mM×0.2ml

SF8993-5mg

Retigabine (Potassium Channel开放剂)

5mg

SF8993-25mg

Retigabine (Potassium Channel开放剂)

25mg

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说明书

1份