Mexiletine D6

Mexiletine-d6 (KOE-1173-d6) is deuterium labeled Mexiletine. Mexiletine is an orally effective antiarrhythmic agent which has also been found to be effective for myotonia and neuropathic pain. Mexiletine exerts its efficacy through blocking sodium channels (IC50 : 75±8 μM for tonic block, 23.6±2.8 μM for use-dependent block), therefore can be used for cardiovascular and neurological research[1][2][3][4][5].

[1] Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. DOI:10.1177/1060028018797110
[2] Campbell RW, et al. Mexiletine. N Engl J Med. 1987，316(1):29-34. DOI:10.1056/NEJM198701013160106
[3] De Bellis M, et al. Combined modifications of mexiletine pharmacophores for new lead blockers of Na(v)1.4 channels. Biophys J. 2013，104(2):344-54. DOI:10.1016/j.bpj.2012.11.3830
[4] Nasilli G, et al. Mexiletine reverses oxaliplatin-induced neuropathic pain in rats. J Pharmacol Sci. 2010;112(4):473-6. DOI:10.1254/jphs.10012sc
[5] Egashira N, et al. Mexiletine reverses oxaliplatin-induced neuropathic pain in rats. J Pharmacol Sci. 2010，112(4):473-6. DOI:10.1254/jphs.10012sc