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Fórmula empírica (notación de Hill):
C11H17NO · HCl
Número CAS:
Peso molecular:
215.72
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
EC Number:
250-825-7
MDL number:
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Permítanos ayudarleNombre del producto
Mexiletine hydrochloride, powder
assay
≥98% (GC)
Quality Level
form
powder
color
white to off-white
solubility
methanol: 50 mg/mL
originator
Boehringer Ingelheim
storage temp.
2-8°C
SMILES string
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
Gene Information
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Categorías relacionadas
General description
Mexiletine is a class I B antiarrhythmic and an analog of lidocaine. It has shelf life of 10-12 hours and is metabolized in liver and eliminated post reduction, oxidation deamination or conjugation.
Application
Mexiletine hydrochloride has been used as a sodium channel blocker:
- expressed in chinese hamster ovary cells
- in human embryonic kidney (HEK) cells for whole cell patch-clamp studies
- electrophysiology studies in HEK cells expressing Nav1.7 protein
Biochem/physiol Actions
Mexiletine is a potent sodium channel blocker. It is a cardiac antiarrhythmic and is used as an adjuvant in headache and neuropathic pain Mexiletine is used for treating myotonia in sodium channelopathies and reduces the cardiac action potential depolarization but shows no impact on atrial refractoriness. Its inhibitory effect on sodium channels is effective in treating potassium aggravated myotonia.
Features and Benefits
This compound was developed by Boehringer Ingelheim. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral
Clase de almacenamiento
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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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
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
Erythromelagia: a rare and hard-to-treat condition: a 9-year-old boy responsive to intravenous lidocaine and oral mexilitene.
Francisca Elgueta et al.
Pain medicine (Malden, Mass.), 14(2), 311-312 (2013-02-02)
Mexiletine for treatment of myotonia: a trial triumph for rare disease networks.
Eric P Hoffman et al.
JAMA, 308(13), 1377-1378 (2012-10-04)
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