Synthesis and Toxicopharmacological Evaluation of m-Hydroxymexiletine, the First Metabolite of Mexiletine More Potent Than the Parent Compound on Voltage-Gated Sodium Channels
作者： Alessia Catalano , Jean-François Desaphy , Giovanni Lentini , Alessia Carocci , Antonia Di Mola
DOI: 10.1021/JM201197Z
关键词:
摘要: The first synthesis of m-hydroxymexiletine (MHM) has been accomplished. MHM displayed hNav1.5 sodium channel blocking activity, and tests indicate it to be ∼2-fold more potent than the parent mexiletine have favorable toxicological properties mexiletine. Thus, possible related prodrugs might studied as agents for treatment arrhythmias, neuropathic pain, myotonias in substitution (metabolite switch), which turned out tainted with common toxicity.
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