质量水平
检测方案
≥98% (HPLC)
形式
powder
药品控制
USDEA Schedule V
颜色
white to light brown
溶解性
DMSO: >15 mg/mL
储存温度
room temp
SMILES字符串
FC1=CC=C(CNC2=CC(N)=C(NC(OCC)=O)C=C2)C=C1
InChI
1S/C16H18FN3O2/c1-2-22-16(21)20-15-8-7-13(9-14(15)18)19-10-11-3-5-12(17)6-4-11/h3-9,19H,2,10,18H2,1H3,(H,20,21)
InChI key
PCOBBVZJEWWZFR-UHFFFAOYSA-N
基因信息
human ... KCNQ1(3784) , KCNQ2(3785) , KCNQ3(3786) , KCNQ4(9132) , KCNQ5(56479)
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生化/生理作用
瑞替加滨(依佐加滨)是一种具有抗惊厥活性的 Kv7.2-7.5 (KCNQ2-5)神经元钾通道开放剂。
警示用语:
Danger
危险声明
危险分类
Acute Tox. 3 Inhalation - Acute Tox. 3 Oral - Aquatic Acute 1 - Aquatic Chronic 1
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Postepy higieny i medycyny doswiadczalnej (Online), 67, 973-981 (2013-10-04)
Retigabine belongs to a new generation of antiepileptic drugs. Its mechanism of action is different from that previously known. Retigabine opens potassium channels of subfamily Kv 7, especially Kv 7.2 and Kv 7.3. The drug enhances GABA-ergic transmission. It is
Nature reviews. Drug discovery, 10(10), 729-730 (2011-10-01)
Ezogabine (Potiga; Valeant Pharmaceuticals/GlaxoSmithKline), a potassium channel opener, was approved in June 2011 by the U.S. Food and Drug Administration (F.D.A.) for the adjunctive treatment of partial-onset seizures in adult patients. The same drug was granted marketing authorization for this
Expert review of neurotherapeutics, 12(5), 509-517 (2012-05-04)
Ezogabine/retigabine (RTG) is a novel antiepileptic compound that activates a voltage-sensitive neuronal-specific outward potassium current that decreases neuronal excitability. RTG has been evaluated in three pivotal placebo-controlled randomized trials as adjunctive therapy in adult drug-resistant partial epilepsy. In comparison to
Clinical therapeutics, 34(9), 1845-1856 (2012-08-25)
Ezogabine, also known as retigabine, is a recently approved anticonvulsant medication with a novel mechanism of action. It activates low-threshold voltage-gated potassium channels, leading to hyperpolarization of the membrane potential, stabilization of the resting membrane potential, and suppression of repetitive
Molecular pharmacology, 86(3), 330-341 (2014-06-20)
Recent research suggests that smooth muscle cells express Kv7.4 and Kv7.5 voltage-activated potassium channels, which contribute to maintenance of their resting membrane voltage. New pharmacologic activators of Kv7 channels, ML213 (N-mesitybicyclo[2.2.1]heptane-2-carboxamide) and ICA-069673 N-(6-chloropyridin-3-yl)-3,4-difluorobenzamide), have been reported to discriminate among
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