SML0325
瑞替加滨
≥98% (HPLC)
别名:
D-23129, N-（2-氨基-4-（4-氟苄基氨基）苯基）氨基甲酸乙酯, 依佐加滨
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关于此项目
经验公式（希尔记法）:
C16H18FN3O2
化学文摘社编号:
分子量:
303.33
UNSPSC Code:
12352200
NACRES:
NA.77
PubChem Substance ID:
MDL number:
Beilstein/REAXYS Number:
8072099
产品名称
瑞替加滨, ≥98% (HPLC)
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)
SMILES string
FC1=CC=C(CNC2=CC(N)=C(NC(OCC)=O)C=C2)C=C1
InChI key
PCOBBVZJEWWZFR-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
drug control
USDEA Schedule V
color
white to light brown
solubility
DMSO: >15 mg/mL
storage temp.
room temp
Quality Level
Gene Information
human ... KCNQ1(3784), KCNQ2(3785), KCNQ3(3786), KCNQ4(9132), KCNQ5(56479)
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Biochem/physiol Actions
瑞替加滨是一种 Kv7.2-7.5 钾通道激活剂； 抗惊厥药。
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。
signalword
Danger
hcodes
Hazard Classifications
Acute Tox. 3 Inhalation - Acute Tox. 3 Oral - Aquatic Acute 1 - Aquatic Chronic 1
存储类别
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Carl E Stafstrom et al.
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
Sylvain Rheims et al.
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
Ewa Zwierzyńska et al.
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
Piotr Czuczwar et al.
Pharmacological reports : PR, 62(2), 211-219 (2010-05-29)
Retigabine represents an antiepileptic drug possessing a completely different mechanism of action when compared to the existing classical and newer antiepileptic drugs. In the therapeutic range, retigabine enhances potassium currents, very likely via destabilization of a closed conformation or stabilization
G Blackburn-Munro et al.
CNS drug reviews, 11(1), 1-20 (2005-05-04)
Retigabine [D23129; N-(2-amino-4-(4-fluorobenzylamino)-phenyl)carbamic acid ethyl ester] is an antiepileptic drug with a recently described novel mechanism of action that involves opening of neuronal K(V)7.2-7.5 (formerly KCNQ2-5) voltage-activated K(+) channels. These channels (primarily K(V)7.2/7.3) enable generation of the M-current, a subthreshold
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