M2727
美西律 盐酸盐
≥98% (GC), powder, sodium channel blocker
别名:
1-(2,6-二甲基苯氧基)-2-丙胺 盐酸盐, 1-(2,6-二甲基苯氧基)-2-丙胺盐酸盐 盐酸盐
产品名称
美西律 盐酸盐, powder
方案
≥98% (GC)
质量水平
表单
powder
颜色
white to off-white
溶解性
methanol: 50 mg/mL
创始人
Boehringer Ingelheim
储存温度
2-8°C
SMILES字符串
Cl[H].CC(N)COc1c(C)cccc1C
InChI
1S/C11H17NO.ClH/c1-8-5-4-6-9(2)11(8)13-7-10(3)12;/h4-6,10H,7,12H2,1-3H3;1H
InChI key
NFEIBWMZVIVJLQ-UHFFFAOYSA-N
基因信息
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相关类别
一般描述
美西律是一种IB类抗心律失常药，是利多卡因的类似物。它的半衰期为10-12小时，在肝脏中代谢，通过还原、氧化或结合反应消除。
应用
盐酸美西律可作为钠离子通道阻滞剂用于：
- 中国仓鼠卵细胞
- 人胚胎肾 (HEK) 细胞，用于全细胞膜片钳研究
- 表达Nav1.7蛋白的HEK细胞的电生理研究
生化/生理作用
美西律是一种有效的钠离子通道阻滞药。它是一种抗心律失常药，在头疼和神经性疼痛中可作为辅助药物美西律用于治疗钠离子通道病的肌强直症状，并缩短心脏动作电位的去极化时程，但不会对心房不应期造成影响。它对钠通道的抑制作用可有效治疗钾加重性肌强直。
特点和优势
该化合物由 Boehringer Ingelheim 开发。想要浏览其他由制药公司开发的化合物以及已批准药物/候选药物清单，请单击此处。
警示用语：
Warning
危险声明
危险分类
Acute Tox. 4 Oral
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
E L Logigian et al.
Neurology, 74(18), 1441-1448 (2010-05-05)
To determine if mexiletine is safe and effective in reducing myotonia in myotonic dystrophy type 1 (DM1). Myotonia is an early, prominent symptom in DM1 and contributes to decreased dexterity, gait instability, difficulty with speech/swallowing, and muscle pain. A few
J F Desaphy et al.
Neuromuscular disorders : NMD, 9(3), 182-189 (1999-06-26)
The sea anemone toxin ATX II impairs skeletal muscle sodium channel inactivation, mimicking the persistent inward current observed in patients suffering from sodium channel myotonia. Mexiletine has beneficial effects on myotonia. To verify the efficiency of the drug on persistent
Min-Tzu Wu et al.
PloS one, 8(1), e55212-e55212 (2013-02-06)
Primary erythromelalgia (PE) is an autosomal dominant neurological disorder characterized by severe burning pain and erythema in the extremities upon heat stimuli or exercise. Mutations in human SCN9A gene, encoding the α-subunit of the voltage-gated sodium channel, Na(v)1.7, were found
Mexiletine
Monk, Jon P and Brogden, Rex N
Drugs, 40(3), 374-411 (1990)
K Mori et al.
Naunyn-Schmiedeberg's archives of pharmacology, 358(6), 641-648 (1999-01-08)
Recently we have reported that class III antiarrhythmic drugs including amiodarone inhibit the Na+-activated K+ (KNa) channels in isolated cardiac cells. In this study effects of antiarrhythmic drugs having class I and/or IV properties on the single KNa channel current
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