期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 55, 期 3, 页码 1418-1422出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm201197z
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资金
- Italian Ministero dell'Istruzione, dell'Universita e della Ricerca [MIUR 2005033023-001]
- French Association Francaise contre les Myopathies [15020]
The first synthesis of m-hydroxymexiletine (MHM) has been accomplished. MHM displayed hNav1.5 sodium channel blocking activity, and tests indicate it to be similar to 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.
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