Searching for new antiarrhythmic agents: Evaluation of meta-hydroxymexiletine enantiomers

摘要: Mexiletine is a very well-known class IB antiarrhythmic drug, whose enantiomers differ in both pharmacodynamic and pharmacokinetic properties, the (R)-isomer being eutomer on experimental arrhythmias binding studies cardiac voltage-gated sodium channels. meta-Hydroxymexiletine (MHM) minor metabolite of mexiletine, which has demonstrated to be more potent than parent compound. Herein we report synthesis biological evaluation MHM for their potential activity. The same stereoselectivity pattern observed mexiletine was found MHM: (R)-enantiomer ac-arrhythmia also showing negative inotropism higher one displayed by and, at time, decreased vasorelaxant activity guinea-pig left atrium ileum longitudinal smooth muscle.