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• W2161004893 abstract "Several macrolides have been reported to cause QT prolongation and ventricular arrhythmias such as torsades de pointes. To clarify the underlying ionic mechanisms, we examined the effects of six macrolides on the human <i>ether-a-go-go</i>-related gene (<i>HERG</i>)-encoded potassium current stably expressed in human embryonic kidney-293 cells. All six drugs showed a concentration-dependent inhibition of the current with the following IC₅₀ values: clarithromycin, 32.9 μM; roxithromycin, 36.5 μM; erythromycin, 72.2 μM; josamycin, 102.4 μM; erythromycylamine, 273.9 μM; and oleandomycin, 339.6 μM. A metabolite of erythromycin, des-methyl erythromycin, was also found to inhibit <i>HERG</i> current with an IC₅₀ of 147.1 μM. These findings imply that the blockade of <i>HERG</i> may be a common feature of macrolides and may contribute to the QT prolongation observed clinically with some of these compounds. Mechanistic studies showed that inhibition of <i>HERG</i>current by clarithromycin did not require activation of the channel and was both voltage- and time-dependent. The blocking time course could be described by a first-order reaction between the drug and the channel. Both binding and unbinding processes appeared to speed up as the membrane was more depolarized, indicating that the drug-channel interaction may be affected by electrostatic responses." @default.
• W2161004893 created "2016-06-24" @default.
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• W2161004893 date "2002-07-01" @default.
• W2161004893 modified "2023-10-02" @default.
• W2161004893 title "Blockade of Human Cardiac Potassium Channel Human <i>Ether-a-go-go-</i>Related Gene (<i>HERG</i>) by Macrolide Antibiotics" @default.
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• W2161004893 doi "https://doi.org/10.1124/jpet.302.1.320" @default.
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