产品名称
美西律 盐酸盐, powder
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
SMILES string
Cl[H].CC(N)COc1c(C)cccc1C
assay
≥98% (GC)
form
powder
color
white to off-white
solubility
methanol: 50 mg/mL
originator
Boehringer Ingelheim
storage temp.
2-8°C
Quality Level
Gene Information
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相关类别
Application
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
Biochem/physiol Actions
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。
Features and Benefits
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。
General description
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。
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_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
Arnold E Pfahnl et al.
Heart rhythm, 4(1), 46-53 (2007-01-03)
Brugada and long QT type 3 syndromes are linked to sodium channel mutations and clinically cause arrhythmias that lead to sudden death. We have identified a novel threonine-to-isoleucine missense mutation at position 353 (T353I) adjacent to the pore-lining region of
Mexiletine
Monk, Jon P and Brogden, Rex N
Drugs, 40(3), 374-411 (1990)
Adam Romman et al.
Pain physician, 21(5), E573-E579 (2018-10-05)
Intravenous lidocaine has multiple applications in the management of acute and chronic pain. Mexiletine, an oral lidocaine analogue, has been used in a number of chronic pain conditions although its use is not well characterized. To report our experience using
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