IndraLab

Statements

reach
"Ivabradine Block of the WT-hERG1 Occurs Through the Extracellular Milieu."
32694995
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"A possible lipophilic access route has been established for ivabradine blockade of hERG in a recent study that implicated a lipid facing residue (M651) as critical for drug induced blockade."
29449809
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"5 The present study demonstrates unequivocally that ivabradine can inhibit hERG, with an IC 50 of = ~ 2 to 3 mumol/L, concordant with an ability to inhibit native I Kr."
25911606
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"The resulting data demonstrate that ivabradine both inhibits hERG with a potency similar to that reported previously for native I f and cloned HCN channels and, furthermore, at therapeutically relevant levels can produce a delay in ventricular repolarization and changes electrical restitution properties in intact perfused hearts."
25911606
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"These findings demonstrate that ivabradine induces a concentration dependent inhibition of hERG channels with an IC 50 similar to that reported for native I f and HCN channels."
25911606
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"HERG potassium channel inhibition by ivabradine requires channel gating."
26275355
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"Ivabradine, ajmaline and mexiletine inhibited the KCNH2 channel currents, probably underlying their APD prolonging effects."
33023024
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"XREF_BIBR - XREF_BIBR The voltage dependence and " envelope of tails " data in this study indicate that hERG block by ivabradine requires channel gating to occur, with a comparatively modest impact on inhibition of inactivation attenuation, consistent with preferential open (activated) channel block."
25911606
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"HERG potassium channel inhibition by ivabradine may contribute to QT prolongation and risk of torsades de pointes."
26301071
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"Ivabradine blocks hERG and prolongs action potential duration."
25986146
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"HERG potassium channel blockade by the HCN channel inhibitor bradycardic agent ivabradine."
25911606
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"Ivabradine also inhibits hERG channel currents."
34025432
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"Ivabradine Inhibits I hERG."
25911606
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"Disruption of C-type inactivation also suppressed block of hERG1 by ivabradine."
25986146
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"In this work, we show the ivabradine block of the hERG1 occurs from the extracellular milieu and little block of the channel is observed during the intracellular application of the drug (XREF_FIG)."
32694995
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"The concentration response relation for ivabradine inhibition of hERG 1a/1b I hERG is also included in XREF_FIG B, with a derived IC 50 of 3.31 mumol/L (CI : 2.97 to 3.70); and n H of 1.06 (CI : 0.93 to 1.19)."
25911606
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"Ivabradine, ajmaline and mexiletine inhibited KCNH2 channel currents significantly, which may underlie their APD prolonging effects."
30947366
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"Results : Ajmaline, amiodarone, ivabradine, flecainide, quinidine, mexiletine and ranolazine inhibited the hERG channel current (I Kr) less strongly in hiPSC-CMs from the SQTS1-patient (SQT1-hiPSC-CMs) comparing with cells from the healthy donor (donor-hiPSC-CMs)."
34025432