IndraLab

Statements

Amiodarone inhibits KCNH2. 29 / 30
12 | 17
ctd
No evidence text available
15821840
ctd
No evidence text available
15618689
ctd
No evidence text available
24052561
reach
"Amiodarone, azimilide, dofetilide, quinidine and sotalol all produced a dose dependent inhibition of HERG current."
16960444
ctd
No evidence text available
18057881
reach
"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
reach
"Amiodarone has been reported to block hERG channels expressed in Xenopus oocytes in closed, open, and inactivated states XREF_BIBR."
27256139
ctd
No evidence text available
11238279
ctd
No evidence text available
16971508
reach
"Amiodarone blocks hERG and prolongs the QT interval, but is a rare cause of TdP (Yang et al., 2001)."
19027781
ctd
No evidence text available
15272206
reach
"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
reach
"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
ctd
No evidence text available
10208308
reach
"Amiodarone blocked HERG channels with an IC50 of 9.8 microM with a maximum outward tail current reduction of 62.8%."
10208308
reach
"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
reach
"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
ctd
No evidence text available
18329740
reach
"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
reach
"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
reach
"These results indicate that HERG channels can be blocked by amiodarone in closed, open and inactivated states."
10208308
reach
"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
ctd
No evidence text available
18724381
reach
"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
reach
"Amiodarone inhibited HERG K+ and late Na+ currents with IC50s of 0.8 +/- 0.1 and 3.0 +/- 0.9 microM, respectively."
18006430
ctd
No evidence text available
16960444
reach
"Vice versa, amiodarone attenuates hERG1 activation by KB130015."
20097192
ctd
No evidence text available
15671647
reach
"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