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Mexiletine activates mutated SCN5A. 3 / 3
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"This is remarkable, since genetic defects in the voltage gated channel SCN5A have been found in a subset of patients with IBS, and normal stool frequency was restored in a severely constipated SCN5A mutant carrier treated with mexiletine, a drug able to rescue SCN5A expression."
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"The only one alive, currently at age 3, carries one of the functionally most severe SCN5A mutations 14 and is treated with beta-blockers, mexiletine, and ventricular pacing."
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"However, some reports have shown that mexiletine, a drug used to inhibit persistent sodium current and to shorten QT interval, rescues trafficking in defective SCN5A mutants (Valdivia et al., 2002; Ruan et al., 2010)."
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