3-hydroxymexiletine and Ataxia

3-hydroxymexiletine has been researched along with Ataxia* in 1 studies

Other Studies

1 other study(ies) available for 3-hydroxymexiletine and Ataxia

Article	Year
Synthesis and toxicopharmacological evaluation of m-hydroxymexiletine, the first metabolite of mexiletine more potent than the parent compound on voltage-gated sodium channels. Journal of medicinal chemistry, 2012, Feb-09, Volume: 55, Issue:3 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 and to have more favorable toxicological properties than mexiletine. Thus, MHM and possible related prodrugs might be studied as agents for the treatment of arrhythmias, neuropathic pain, and myotonias in substitution of mexiletine (metabolite switch), which has turned out to be tainted with common toxicity. Topics: Animals; Anti-Arrhythmia Agents; Aorta; Ataxia; ATP Binding Cassette Transporter, Subfamily B, Member 1; Blood-Brain Barrier; Caco-2 Cells; Guinea Pigs; Heart; Heart Rate; HEK293 Cells; Humans; Ion Channel Gating; Mexiletine; Mice; NAV1.5 Voltage-Gated Sodium Channel; Permeability; Sodium Channels; Stereoisomerism; Vasodilator Agents	2012

Article

Year

Synthesis and toxicopharmacological evaluation of m-hydroxymexiletine, the first metabolite of mexiletine more potent than the parent compound on voltage-gated sodium channels.

Journal of medicinal chemistry, 2012, Feb-09, Volume: 55, Issue:3

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 and to have more favorable toxicological properties than mexiletine. Thus, MHM and possible related prodrugs might be studied as agents for the treatment of arrhythmias, neuropathic pain, and myotonias in substitution of mexiletine (metabolite switch), which has turned out to be tainted with common toxicity.

Topics: Animals; Anti-Arrhythmia Agents; Aorta; Ataxia; ATP Binding Cassette Transporter, Subfamily B, Member 1; Blood-Brain Barrier; Caco-2 Cells; Guinea Pigs; Heart; Heart Rate; HEK293 Cells; Humans; Ion Channel Gating; Mexiletine; Mice; NAV1.5 Voltage-Gated Sodium Channel; Permeability; Sodium Channels; Stereoisomerism; Vasodilator Agents

2012