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Mexiletine hydrochloride

Mexiletine hydrochloride 구조식 이미지
카스 번호:
5370-01-4
상품명:
Mexiletine hydrochloride
동의어(영문):
Toy;Katen;ko1173;Olzoron;mexitil;Ritalmex;Ko 1173Cl;Mexilitene;Cirumimeru;MEXILITINE HCL
CBNumber:
CB6114224
분자식:
C11H18ClNO
포뮬러 무게:
215.72
MOL 파일:
5370-01-4.mol

Mexiletine hydrochloride 속성

녹는점
200-203°C
밀도
1.12 g/cm3
저장 조건
2-8°C
용해도
ethanol: 50 mg/mL
산도 계수 (pKa)
9.0(at 25℃)
물리적 상태
powder
색상
white
최대 파장(λmax)
272nm(MeOH)(lit.)
Merck
14,6169
CAS 데이터베이스
5370-01-4(CAS DataBase Reference)
안전
  • 위험 및 안전 성명
  • 위험 및 사전주의 사항 (GHS)
위험품 표기 Xn
위험 카페고리 넘버 20/21/22-36/37/38-22
안전지침서 36-26
WGK 독일 3
RTECS 번호 KR9300000
HS 번호 2922190900
독성 LD50 in male, female rats, mice, rabbits (mg/kg): 350, 400, 310, 400, 180, 160 orally; in male, female rats, mice (mg/kg): 27, 30, 43, 50 i.v. (Kast)
기존화학 물질 KE-11772
그림문자(GHS):
신호 어: Warning
유해·위험 문구:
암호 유해·위험 문구 위험 등급 범주 신호 어 그림 문자 P- 코드
H302 삼키면 유해함 급성 독성 물질 - 경구 구분 4 경고 P264, P270, P301+P312, P330, P501
예방조치문구:

Mexiletine hydrochloride C화학적 특성, 용도, 생산

개요

Mexiletine is a voltage-gated sodium channel blocker and class Ib antiarrhythmic agent that preferentially binds to open/inactive channels. It inhibits aconitine-induced dysrhythmias in mice with ED50 values of 57 and 107 mg/kg for intraperitoneal and oral administration, respectively. Mexiletine decreases or inhibits conduction across the Purkinje fiber-muscle junction, shortens action potential duration, and decreases the refractory period when used at concentrations less than 5 μg/ml in isolated canine Purkinje fiber and ventricular muscle preparations.

화학적 성질

White to Off-White Solid

Originator

Mexitil,Boehringer Ingelheim,US,1976

용도

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

용도

Antiarrhythmic (class IB)

용도

antipsychotic

정의

ChEBI: A hydrochloride composed of equimolar amounts of mexiletine and hydrogen chloride.

Manufacturing Process

The sodium salt of dimethyl phenol was reacted with chloroacetone and this product with hydroxylamine to give the starting material.
245 g of this 1-(2',6'-dimethyl-phenoxy)-propanone-(2)-oxime were dissolved in 1,300 cc of methanol, and the solution was hydrogenated at 5 atmospheres gauge and 60°C in the presence of Raney nickel. After the calculated amount of hydrogen had been absorbed, the catalyst was filtered off, the methanol was distilled out of the filtrate,and the residue, raw 1-(2',6'-dimethylphenoxy)-2-amino-propane, was dissolved in ethanol. The resulting solution was acidified with ethereal hydrochloric acid, the acidic solution was allowed to cool, and the precipitate formed thereby was collected by vacuum filtration. The filter cake was dissolved in ethanol and recystallized therefrom by addition of ether. 140.5 g (51.5% of theory) of a substance having a melting point of 203°C to 205°C were obtained, which was identified to be 1-(2',6'- dimethyl-phenoxy)-2-anino-propane hydrochloride.

상표명

Mexitil (Boehringer Ingelheim).

Therapeutic Function

Antiarrhythmic

일반 설명

Mexiletine hydrochloride,1-methyl-2-(2,6-xylyloxy)ethylamine hydrochloride (Mexitil)(pKa 8.4), is a class IB antiarrhythmic agent that is effectivewhen given either intravenously or orally. It resembles lidocainein possessing a xylyl moiety but otherwise is differentchemically. Mexiletine hydrochloride is an ether and is notsubject to the hydrolysis common to the amides lidocaineand tocainide. Its mean half-life on oral administration isapproximately 10 hours.
Although not subject to hydrolysis, mexiletine hydrochlorideis metabolized by oxidative and reductiveprocesses in the liver. Its metabolites, p-hydroxymexiletineand hydroxymethylmexiletine, are not pharmacologicallyactive as antiarrhythmic agents.

생물학적 활성

Use-dependent sodium channel blocker (IC 50 values are 75.3 and 23.6 μ M for tonic and use-dependent block respectively). Class Ib antiarrhythmic, neuroprotective and antimyotonic agent.

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.

Clinical Use

Mexiletine hydrochloride, like class I antiarrhythmicagents, blocks the fast Na channel in cardiac cells. It isespecially effective on the Purkinje fibers in the heart. Thedrug increases the threshold of excitability of myocardialcells by reducing the rate of rise and amplitude of the actionpotential and decreases automaticity.
Mexiletine hydrochloride is used for long-term oral prophylaxisof ventricular tachycardia. The drug is given in200- to 400-mg doses every 8 hours.

Mexiletine hydrochloride 준비 용품 및 원자재

원자재

준비 용품


Mexiletine hydrochloride 공급 업체

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Target Molecule Corp
18019718960 781-999-5354
marketing@targetmol.com United States 19231 58

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