Key result
Amitriptyline dose-dependently blocked HERG channels (IC50 3.26 microM at +20 mV) and reduced I(Kr) in rat atrial myocytes by 55% at 5 microM, explaining its arrhythmogenic side effects.
Population
Xenopus oocytes expressing human ether-a-go-go-related gene (HERG) channels and rat atrial myocytes
Design
Preclinical
Authors
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Amitriptyline blocks HERG/IKr, potentially raising arrhythmia risk; leaves open clinical translation and human cardiomyocyte effects.
Amitriptyline blocks HERG potassium channels in a dose-, voltage-, and use-dependent manner, providing a mechanistic basis for its known arrhythmogenic side effects like QT prolongation.
Jo et al. (2000) studied this question. Amitriptyline was evaluated on HERG channel and I(Kr) current blockade. Amitriptyline dose-dependently blocked HERG channels (IC50 3.26 microM at +20 mV) and reduced I(Kr) in rat atrial myocytes by 55% at 5 microM, explaining its arrhythmogenic side effects.
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