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Fluphenazine inhibits KCNH2. 11 / 11
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"This indicates that the hERG channels were only slightly blocked by fluphenazine while remaining at the holding potential."
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"In order to address whether hERG channels are also blocked by fluphenazine in their inactivated state, a long test pulse to +80 mV (4 s) was applied to inactivate the channels, which was followed by a[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"However, the biophysical properties and molecular determinants for the fluphenazine block of the hERG channel have not been reported.In this study, we examined the possible fluphenazine block of hERG [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"Overall, fluphenazine inhibits the hERG channels mainly in the open and inactivated state rather than in the closed state.The IC 50 values of many hERG channel blockers have been shown to differ depen[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"The potency of a channel block for the wild type and mutant hERG channel (Y652A) were compared in order to determine if the key residue is also important in the fluphenazine-induced blocking of the hE[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"As for the effect of the drug on cardiac rhythmicity, the drug was identified as significant predictor for QT prolongation ( Chong et al., 2003; Turbott et al., 1987 ) and is known to induce the life-[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"Therefore, the possible accumulated concentration of fluphenazine may be assumed to be in the range from 40 to 108 nM in the heart, which is comparable with our findings that fluphenazine at 0.1 μM pr[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"Our present results support that the direct inhibition of hERG by fluphenazine would be a major cause of APD prolongation because the pore mutation (Y652A) of the channel protein significantly attenua[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"Another view of the voltage dependence of a fluphenazine block of the hERG channels is that the drug may increase the APD and make the heart more prone to arrhythmia, particularly under the pathologic[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"Therefore the docking result of fluphenazine to the hERG channel is consistent with the model that we have proposed.In conclusion, we found that the antipsychotic drug fluphenazine directly prolongs A[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"For example, the antipsychotic fluphenazine directly inhibits human ether-a-go-go-related gene (hERG) K + channels in a voltage- and time-dependent manner ( Hong et al., 2013 )."
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