IndraLab

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Moxifloxacin inhibits KCNH2. 23 / 23
2 | 21
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"Because the ability of moxifloxacin to inhibit HERG channels is unknown, this study explored the effect of moxifloxacin on HERG channel currents and glucose metabolism in mice."
26649323
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"In common with other QT prolonging agents, moxifloxacin is known to inhibit the hERG potassium K+ channel, but at present there is little mechanistic information available on this action."
16474415
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"In contrast, moxifloxacin blocked HERG current amplitude with an IC50 value of 74.7 microM."
14512100
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"At standard clinical concentrations moxifloxacin induces approximately 5% hERG potassium channel block and 10 ms of QTc prolongation, and in our clinical study a supratherapeutic dose of intravenous moxifloxacin caused a QTc prolongation of 30 ms. At similar concentrations, the iPSC cardiomyocytes did not show statistically significant APDc or FPDc prolongation, but moxifloxacin caused concentration dependent APDc and FPDc prolongation above this range (21-200 muM), and arrhythmias were detected in in both cell types at approximately 50-fold clinical Cmax."
27701120
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"Bath application of sparfloxacin, moxifloxacin and grepafloxacin produced an inhibition of HERG outward currents at -40 mV with EC (50) of 13.5 +/-0.8, 41."
11040340
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"Alexandrou AJ, Duncan RS, Sullivan A, et al. Mechanism of hERG K+ channel blockade by the fluoroquinolone antibiotic moxifloxacin."
34471515
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"Grepafloxacin and moxifloxacin suppressed the HERG current with EC 50 of 37.5 +/-3.3 mug/ml and 41.2 +/-2.0 mug/ml and n H = 1.4 +/-0.2 and 1.1 +/-0.1, respectively."
11040340
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"Ciprofloxacin was found to have little interaction with the HERG channel at concentrations up to 100 mug/ml, whilst sparfloxacin, grepafloxacin and moxifloxacin inhibited HERG currents with IC 50 valu[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
11040352
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"The same was true for other hERG channel blockers (like erythromycin, moxifloxacin and sematilide) and multi-ion channel blockers."
29311989
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No evidence text available
24052561
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"Moxifloxacin Induced Inhibition of the HERG Channel in HEK293 Cells."
26649323
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"In contrast, moxifloxacin clearly blocked HERG current amplitude with an IC 50 value of 74.7 muM."
14512100
ctd
No evidence text available
27553911
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"Block of hERG by moxifloxacin was found to be voltage dependent, occurred rapidly and was independent of stimulation frequency."
16474415
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"Moxifloxacin inhibited the hERG current with an IC50 of 35.7 microM."
16158069
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"Indeed, moxifloxacin (40), fluvoxamine (41), and, recently, doxepin (42) have been reported to inhibit hERG with a mixed state-dependence of inhibition (with components of both closed- and open-channe[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
19720020
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"The comparison of potencies from grepafloxacin, moxifloxacin, and sparfloxacin to block the HERG channel shows the latter to have the greatest inhibition effect on the HERG current amplitude."
11040340
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"Mechanistically, moxifloxacin treatment and LQT-2 patients share a common pathophysiology in that moxifloxacin blocks the hERG potassium channel XREF_BIBR and LQT2 patients have mutations in the gene encoding the hERG channel XREF_BIBR, XREF_BIBR."
24454918
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"Our data demonstrate that moxifloxacin blocks the hERG channel with a preference for the activated channel state."
16474415
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"In contrast, moxifloxacin blocked HERG current amplitude with an IC 50 value of 74.7 muM."
14512100
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"The Tyr652 but not Phe656 S6 residue is involved in moxifloxacin block of hERG, concordant with an interaction in the channel inner cavity."
16474415
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"We demonstrated that the time dependent and tail currents for HERG decreased in response to 100mumol/L of moxifloxacin indicating that moxifloxacin inhibits the HERG channel in HEK293 cells."
26649323
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"Our data demonstrate that hERG channel blockers, such as E4031 and moxifloxacin, prolonged field potential duration (FPD) at low concentration and induced arrhythmic beating activity as measured by field potential (FP) recording and impedance (IMP) recordings at higher concentrations."
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