摘要
托卡宁是一种抗心律失常药,属于ib类,主要用于抑制有症状的室性心律失常。据报道,托卡宁还可减轻抽搐、人类三叉神经痛和耳鸣等疼痛。腹腔注射托卡宁后,观察到明显的抗伤害作用,如热板试验所测定的。到20世纪80年代中期,托卡宁作为一种更为有效的治疗肌强直性疾病的药物出现。许多严重不良反应的报告导致停止使用托卡宁,尽管对托卡宁及其类似物的研究,赋予了更好的药理学特征,但仍在进行中,因为它们在肌张力治疗中的潜在作用。本文综述了近几十年来发展起来的外消旋和光学活性托卡宁的不同合成路线,以及对映体分离方法的分析研究。最后,文献中还提到了一些类似于托卡宁的药物,其中大部分是药理学研究中提到的。
关键词: 抗心律失常药,抗肌强直药,钠通道阻滞剂,托卡宁,HNAV1.4,肌强直。
Current Medicinal Chemistry
Title:A Focus on the Synthesis and Pharmacokinetics of Tocainide and its Analogues
Volume: 25 Issue: 42
关键词: 抗心律失常药,抗肌强直药,钠通道阻滞剂,托卡宁,HNAV1.4,肌强直。
摘要: Tocainide is an antiarrhythmic agent belonging to class IB that was primarily used for suppression of symptomatic ventricular arrhythmias. Tocainide was also reported to relieve pain such as tic douloureux, trigemina neuralgia in humans and tinnitus. Significant antinociception, as assayed on the hot-plate test, was observed after intraperitoneal injection of tocainide, too. By the mid-1980s tocainide was emerging as a more consistently effective treatment for myotonic disorders. Numerous reports of serious adverse reactions led to the use of tocainide being discontinued, even though research on tocainide and its analogues, endowed with a better pharmacological profile, is still in progress for their potential usefulness in the treatment of myotonias. This review is focused on the description of the different synthetic routes to racemic and optically active tocainide developed in the last decades, as well as analytical studies regarding enantioseparation methods. Finally, some analogues of tocainide reported in the literature, most of which with pharmacological studies, have been mentioned.
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Cite this article as:
A Focus on the Synthesis and Pharmacokinetics of Tocainide and its Analogues, Current Medicinal Chemistry 2018; 25 (42) . https://dx.doi.org/10.2174/0929867325666180327104320
DOI https://dx.doi.org/10.2174/0929867325666180327104320 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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