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.
Export Options
About this article
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 |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Approaches to the treatment of chronic inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...read more
![Wayfinder Image](/images/wayfinder.jpg)
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Role of Genomic Alterations in HER2 Positive Breast Carcinoma: Focus on Susceptibility and Trastuzumab-therapy
Current Cancer Drug Targets Clinical Trials of Targeted Alpha Therapy for Cancer
Reviews on Recent Clinical Trials A Novel Information Theoretic Approach to Gene Selection for Cancer Classification Using Microarray Data
Current Bioinformatics DoE Based Optimization and Development of Spray-Dried Chitosan-Coated Alginate Microparticles Loaded with Cisplatin for the Treatment of Cervical Cancer
Current Molecular Pharmacology Soft Bipolar Spectrum and Staging in Bipolar Disorder
Current Psychiatry Reviews Superior Anticancer Potential of Nano-Paclitaxel Combined Bevacizumab Treatment in Ovarian Cancer
Current Pharmaceutical Biotechnology Current Progress of Reelin in Development, Inflammation and Tissue Remodeling: From Nervous to Visual Systems
Current Molecular Medicine Signaling Pathways of the ING Proteins in Apoptosis
Current Drug Targets Nano-carrier Polyamidoamine Dendrimer G4 Induces Mitochondrialdependent Apoptosis in Human Multidrug-resistant Breast Cancer Cells through G0/G1 Phase Arrest
Current Pharmaceutical Biotechnology Recognition and Function of HumanγδT Cells: Application for Tumor Immunotherapy
Current Immunology Reviews (Discontinued) Recent Advances in Small Molecule Inhibitors of VEGFR and EGFR Signaling Pathways
Current Topics in Medicinal Chemistry Implications of Nanotechnology in Healthcare
Nanoscience & Nanotechnology-Asia Synthesis of Novel Steroid Derivatives Derived from Dehydroepiandrosterone as Potential Anticancer Agents
Anti-Cancer Agents in Medicinal Chemistry Synthesis of New Curcumin-like Pentadienones by O- and C-glycosylation
Current Organic Chemistry Click Synthesis, Anticancer Activity and Molecular Docking Studies on Pyridazinone Scaffolds
Current Organic Chemistry Specific Targeted Therapy: A New Tool for the Destruction of Cancer
Current Drug Therapy Prodrug Design of Phenolic Drugs
Current Pharmaceutical Design A Proteomic Analysis of Human Uterine Myoma
Current Protein & Peptide Science The Therapeutic Potential of Targeting the Toll-like Receptor Pathway in Breast Cancer
Current Pharmaceutical Design Lipid Rafts and Fas/CD95 Signaling in Cancer Chemotherapy
Recent Patents on Anti-Cancer Drug Discovery