IndraLab

Statements

Amiodarone inhibits KCNH2. 19 / 32
12 | 19
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"In XREF_FIG we can compare the results of the two types of inference for real data on amiodarone block of the hERG current."
27918599
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"Amiodarone inhibited HERG K+ and late Na+ currents with IC50s of 0.8 +/- 0.1 and 3.0 +/- 0.9 microM, respectively."
18006430
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"Amiodarone blocked HERG channels with an IC50 of 9.8 microM with a maximum outward tail current reduction of 62.8%."
10208308
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"Since they are targets of various drugs with cardiac side effects we tested whether the amiodarone derivative 2-methyl-3-(3,5-diiodo-4-carboxymethoxybenzyl) benzofuran (KB130015) blocks hERG1 channels like its parent compound."
20097192
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"Amiodarone blocks hERG and prolongs the QT interval, but is a rare cause of TdP (Yang et al., 2001)."
19027781
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"In order to test whether the amiodarone derivative KB130015 (2-methyl-3-(3,5-diiodo-4-carboxymethoxybenzyl) benzofuran, XREF_BIBR) blocks hERG1 channels similarly, we expressed hERG1 in HEK 293 cells and measured whole-cell currents using the patch-clamp technique."
20097192
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"HERG current in oocytes was reduced by amiodarone (IC (50) = 38 micromol/L), whereas KvLQT1 and minK current was unaffected by 300 micromol/L amiodarone."
11238279
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"These results indicate that HERG channels can be blocked by amiodarone in closed, open and inactivated states."
10208308
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"As shown in XREF_FIG, 1 muM amiodarone blocked hERG1 channels of oocytes pretreated with the vehicle (0.1% DMSO) to 55.6 +/- 5.5% (n = 6) of the control current."
20097192
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"Amiodarone blocked the hERG currents in a concentration-dependent manner with an IC 50 of 4.3 μM and a Hill coefficient of 1.0 ( Fig. 2 C), implying that a single molecule mediates the channel block."
22020101
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"These observations raise the possibility that binding determinants of amiodarone inhibition of hERG channels may be qualitatively or quantitatively different from those for canonical high affinity hERG inhibitors."
27256139
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"A prior study, conducted utilising Xenopus oocyte expression, has suggested that hERG channel inhibition by amiodarone exhibits both gated-state and closed-state components XREF_BIBR."
27256139
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"Amiodarone has been reported to block hERG channels expressed in Xenopus oocytes in closed, open, and inactivated states XREF_BIBR."
27256139
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"Vice versa, amiodarone attenuates hERG1 activation by KB130015."
20097192
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"On the other hand, amiodarone blocks the hERG potassium and calcium and sodium channels, resulting in substantial QT prolongation, but carries a very low risk of degenerating into torsade de pointes 60."
28695570
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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
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"Experimental data suggest that F656 and Y652 in the S6 segment and S624 at the base of the selectivity filter (SF) play key roles in the ability of amiodarone to block hERG channels (Zhang et al., 2016)."
38035013
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"KB130015 presumably binds to the hERG1 pore from the cytosolic side and functionally competes with hERG1 block by amiodarone, E4031 (N-[4-[[1-[2-(6-methyl-2-pyridinyl) ethyl] -4-piperidinyl] carbonyl] phenyl] methanesulfonamide dihydrochloride), and sertindole."
20097192
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"Amiodarone, azimilide, dofetilide, quinidine and sotalol all produced a dose dependent inhibition of HERG current."
16960444