IndraLab

Statements

Rosiglitazone inhibits KCNH2. 5 / 5
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"Blockade of human HERG K+ channels by rosiglitazone, an antidiabetic drug."
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"Rosiglitazone did not change the steady-state activation or inactivation curves or the activation or deactivation kinetics, implying that rosiglitazone blocks HERG channels predominantly in the open and inactivated state rather than in the closed state."
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"Rosiglitazone inhibited HERG channels in a concentration dependent manner, with an IC50 value of 18.8 muM and a Hill coefficient of 1.0."
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"The present study suggests that rosiglitazone blocks HERG channels by binding to activated and inactivated channels, and rosiglitazone use should thus be carefully monitored in patients with pre-existing QT prolongation."
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"Such an investigation is warranted since high dose rosiglitazone may inhibit human ether-a-go-go-related gene (hERG) potassium channels (a surrogate for delayed cardiac repolarization [14]) in a human cell line [15]."
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