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].
In Vivo, Mexiletine (30, 100 mg/kg, p.o., acute administration) reverses both mechanical allodynia and cold hyperalgesia in Oxaliplatin induced rats[4].
In Vitro, Mexiletine (10µM, 48 h) increases peak INa and late INa in HEK293A cells transfected with SCN5A-WT or SCN5A-1795insD while Mexiletine (10µM, 5 min) blocks the late INa[3].
References:
[1]. Campbell RW, et al. Mexiletine. N Engl J Med. 1987，316(1):29-34.
[2]. 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.
[3]. Nasilli G, et al. Mexiletine reverses oxaliplatin-induced neuropathic pain in rats. J Pharmacol Sci. 2010;112(4):473-6.
[4]. Egashira N, et al. Mexiletine reverses oxaliplatin-induced neuropathic pain in rats. J Pharmacol Sci. 2010，112(4):473-6.
In Vivo, Mexiletine (30, 100 mg/kg, p.o., acute administration) reverses both mechanical allodynia and cold hyperalgesia in Oxaliplatin induced rats[4].
In Vitro, Mexiletine (10µM, 48 h) increases peak INa and late INa in HEK293A cells transfected with SCN5A-WT or SCN5A-1795insD while Mexiletine (10µM, 5 min) blocks the late INa[3].
References:
[1]. Campbell RW, et al. Mexiletine. N Engl J Med. 1987，316(1):29-34.
[2]. 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.
[3]. Nasilli G, et al. Mexiletine reverses oxaliplatin-induced neuropathic pain in rats. J Pharmacol Sci. 2010;112(4):473-6.
[4]. Egashira N, et al. Mexiletine reverses oxaliplatin-induced neuropathic pain in rats. J Pharmacol Sci. 2010，112(4):473-6.