2013
DOI: 10.1016/j.ejmech.2013.05.008
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Searching for new antiarrhythmic agents: Evaluation of meta-hydroxymexiletine enantiomers

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Cited by 18 publications
(14 citation statements)
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“…At the dose of 50 mg/kg ip, only compound 1e showed a significant impairment of mouse motor coordination, with a slight increase in the number of falls being displayed. Since mexiletine is known to undergo extensive first-pass oxidative metabolism [16,26,27] that is linked to the generation of reactive species metabolites and/or cellular oxidative stress, the cytotoxicity of the four analogues was assessed using the MTT cell viability assay [28]. When the human hepatocellular liver carcinoma cells (HepG2) were challenged with the four mexiletine analogues at two concentrations (the first close to their corresponding EC 50 values, and the second 10-fold higher than the former), no cytotoxicity was observed (data not shown).…”
Section: Biological Resultsmentioning
confidence: 99%
“…At the dose of 50 mg/kg ip, only compound 1e showed a significant impairment of mouse motor coordination, with a slight increase in the number of falls being displayed. Since mexiletine is known to undergo extensive first-pass oxidative metabolism [16,26,27] that is linked to the generation of reactive species metabolites and/or cellular oxidative stress, the cytotoxicity of the four analogues was assessed using the MTT cell viability assay [28]. When the human hepatocellular liver carcinoma cells (HepG2) were challenged with the four mexiletine analogues at two concentrations (the first close to their corresponding EC 50 values, and the second 10-fold higher than the former), no cytotoxicity was observed (data not shown).…”
Section: Biological Resultsmentioning
confidence: 99%
“…Both the prevention of ventricular tachycardia and the tonic block of the skeletal muscle channel effects exerted by ( R )‐mexiletine were higher than those displayed by its enantiomer , . At the same time, the ( S )‐isomer of mexiletine is more effective than the ( R )‐isomer in the treatment of allodynia .…”
Section: Using Direct Methods To Obtain Single Enantiomer Apismentioning
confidence: 99%
“…Elemental analyses were performed on a Eurovector Euro EA 3000 analyzer. Chromatographic separations were performed on silica gel columns by column chromatography on silica gel (Kieselgel 60, 0.040–0.063 mm, Merck, Darmstadt, Germany) as previously described . TLC analyses were performed on precoated silica gel on aluminum sheets (Kieselgel 60 F 254 , Merck).…”
Section: Methodsmentioning
confidence: 99%