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Chloroquine inhibits KCNH2. 23 / 23
| 1 22
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"Similarly, exposure to 3 µM erythromycin or 30 µM erythromycin was associated with increased hERG block by chloroquine (Table 1)."
32147975
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"Our experimental findings and modeling suggest that chloroquine preferentially blocks open HERG channels by cation-pi and pi stacking interactions with Tyr 652 and Phe 656 of multiple subunits."
11960982
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"The estimated IC 25 -value for chloroquine block of the hERG tail current was 0.3 mug/ml (0.94 muM), the estimated IC 50 -value was 0.8 mug/ml (2.5 muM) and the IC 75 -value for chloroquine block of t[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
14729380
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"Lopinavir, remdesivir, and chloroquine were also shown to have low toxic dose threshold in humans, inhibit human ether-a-go-go-related gene (hERG) and induce hepatotoxicity (Table 5)."
32375574
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"For instance, among COVID-19 treatment drugs, chloroquine and hydroxychloroquine were demonstrated to block hERG potassium channels, whereas azithromycin and remdesivir did not [143] ."
35336980
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"Key Results: Chloroquine and hydroxychloroquine blocked hERG with IC50 of 1.47±0.07 µM and 3.78±0.17 µM respectively, indicating proarrhythmic risk at concentrations effective against SARS-CoV-2 in vitro and proposed in COVID-19 clinical trials."
| DOI
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"Not surprisingly, the treatment of chloroquine, a well described arrhythmogenic drug, significantly inhibited hERG currents with and IC 50 4.5 muM (XREF_FIG B, upper panel) and increased the field potential duration (FPD) of hiPSC-CMs in a dose dependent manner."
| PMC
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"Chloroquine has been shown to inhibit the hERG K + channels in aconcentration- and time dependent manner [XREF_BIBR]."
32351347
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"Chloroquine inhibited the hERG tail current also in a concentration dependent manner, with a significant inhibition of tail current observed at concentrations of> = 0.5 mug/ml."
14729380
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"We found that Chloroquine inhibits hERG, Nav1.5, and Cav1.2 channels, whereas Hydroxychloroquine inhibits hERG and Cav1.2 channels."
33483756
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"XREF_FIG shows that Hydroxychloroquine and Chloroquine inhibited the hERG current with IC50 values of 9.7 and 7.77 microM, respectively, but Azithromycin had no effect."
33483756
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"When erythromycin was applied after steady‐state hERG channel block by thioridazine, dofetilide or chloroquine, erythromycin superfusion was associated with a potentiation of hERG block suggesting independent actions."
32147975
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"Chloroquine and hydroxychloroquine blocked hERG with IC 50 of 1.47±0.07 μM and 3.78±0.17 μM respectively, indicating proarrhythmic risk at concentrations effective against SARS-CoV-2 in vitro."
34837219
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"Significance Statement This work demonstrates that among off-label potential COVID-19 treatment drugs chloroquine, hydroxychloroquine, azithromycin, and remdesivir, the former two drugs block hERG potassium channels while the latter two drugs do not."
33674391
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"As IC 50 values for chloroquine inhibition of both Kir2.1 and hERG seen under our conditions fall within this clinical range, it seems likely that inhibition of both these channel types may contribute to observed QT C interval prolongation."
19285083
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"Chloroquine can be anticipated also to inhibit KCNH2 encoded hERG channel subunits (which underlie native I Kr) [e.g. XREF_BIBR] and in additional experiments (not shown) we found chloroquine to inhibit WT-hERG channels at overlapping concentrations (IC 50 of 2.18 muM; 95% C.I. 1.98 to 2.39 muM; though, in contrast to Kir2.1, blocking potency of the SQT1 linked N588K hERG mutation was reduced ~ 8.5-fold in our hands; data not shown)."
19285083
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"Chloroquine has been shown to block hERG channels with an IC 50 of 2.5 microM."
32888379
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"To a lesser extent, chloroquine also blocks the rapid delayed rectifier Ikr, possibly through cation-pi and pi stacking interactions with tyrosine 652 and phenylalanine 656 in the S6 domain of hERG (Sanchez-Chapula et al., 2002)."
32681537
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"Our results showed that while chloroquine acutely blocked hERG current (I hERG) with an IC 50 of 3.0 microM, hydroxychloroquine acutely blocked I hERG 8-fold less potently, with an IC 50 of 23.4 microM."
33674391
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"Our results showed that while chloroquine acutely blocked hERG current (I hERG) with an IC 50 of 3.0 microM, hydroxychloroquine acutely blocked I hERG 8-fold less potently, with an IC50 of 23.4 microM."
| PMC
eidos
"Chloroquine and hydroxychloroquine blocked hERG with IC 50 of 1.47 + / -0.07 muM and 3.78 + / -0.17 muM respectively , indicating proarrhythmic risk at concentrations effective against SARS-CoV-2 in vitro ."
34837219
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"Chloroquine is a moderate inhibitor of hERG with electrophysiology studies indicating IC 50 values ranging from 2.5 to 19.7 muM, depending on the experimental setting used [XREF_BIBR]."
32316270
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"If multiple ECGs were recorded during chloroquine therapy, the ECG recording which was closest to the time to reach the maximum plasma concentration (T max) of the drug (4-5h after oral administration) was selected, since chloroquine blocks the hERG channel in aconcentration dependent manner and therefore the maximal blocking effect is expected to be at the T max of the drug [XREF_BIBR]."
32351347