IndraLab

Statements

Moxifloxacin inhibits KCNH2. 30 / 32
2 | 30
reach
"In contrast, moxifloxacin clearly blocked HERG current amplitude with an IC 50 value of 74.7 muM."
14512100
reach
"Therefore, in order to contrast the time course of their action, comparison of the relative rates of hERG blockade by Moxifloxacin and Dofetilide was performed at their respective IC50s in the in vitr[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
21419854
reach
"In addition to E4031, some less potent hERG channel inhibitors such as moxifloxacin was also included as part of the evaluation ( Table 2 )."
27282640
reach
"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
reach
"Block of hERG by moxifloxacin was found to be voltage dependent, occurred rapidly and was independent of stimulation frequency."
16474415
reach
"Our data demonstrate that moxifloxacin blocks the hERG channel with a preference for the activated channel state."
16474415
reach
"The Tyr652 but not Phe656 S6 residue is involved in moxifloxacin block of hERG, concordant with an interaction in the channel inner cavity."
16474415
reach
"Moxifloxacin blocks the hERG potassium channel at a clinically relevant IC 50 value (0.93–398 μM) ( Patel et al., 2018 ) and often serves as a positive control for TdP risk."
36343672
reach
"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
reach
"Two hERG-blocking drugs, Dofetilide and Moxifloxacin, were also tested on iPSC derived cardiomyocytes for QT prolongation (201)."
38440211
reach
"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
reach
"Moxifloxacin Induced Inhibition of the HERG Channel in HEK293 Cells."
26649323
reach
"Moxifloxacin inhibited the HERG current with an IC 50 value of 35.7 μM, and moxifloxacin produced roughly 8–10% QT interval prolongation both in arterially perfused rabbit ventricular wedge and in con[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
17027138
reach
"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
reach
"Moxifloxacin has been shown to inhibit the hERG channel ( Bischoff, Schmidt, Netzer, & Pongs, 2000; Kang, Wang, Chen, Triggle, & Rampe, 2001 )."
21419854
reach
"The same was true for other hERG channel blockers (like erythromycin, moxifloxacin and sematilide) and multi-ion channel blockers."
29311989
reach
"In this study, we have tested a known hERG-blocking agent, moxifloxacin, as well as a ß-adrenoceptor blocker, propranolol, in the pig model."
19427912
reach
"Moxifloxacin blocks the HERG channel with a preference for the activated channel state, and the Tyr652 but not Phe656 residue is involved in moxifloxacin block of the HERG channel, concordant with an [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
17027138
reach
"Moxifloxacin and Dofetilide were found to inhibit hERG channels with an IC50 of 71 μM and 6 nM, respectively.To test the hypothesis that the onset time course of hERG blocking effect by Moxifloxacin a[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
21419854
reach
"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
reach
"In contrast, moxifloxacin blocked HERG current amplitude with an IC 50 value of 74.7 muM."
14512100
reach
"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
reach
"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
reach
"Moxifloxacin inhibited the hERG current with an IC50 of 35.7 microM."
16158069
reach
"Unlike many anti-TB drugs, for instance, moxifloxacin and BDQ, both NITD-304 and NITD-349 were devoid of the cardiotoxic liability, as neither of them inhibited the hERG channel (IC > 30 µM)."
36982277
reach
"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
reach
"Increases in QTc and JTpc intervals with administration of the pure hERG blocker moxifloxacin and an initial QTc and JTpc shortening followed by prolongation with the mixed ion channel blocker amiodarone were detected as expected, aligning with clinical data."
38852685
reach
"Experimental data suggest that Y652 and F656 in the S6 segment and S624 at the base of the SF play key roles in the ability of moxifloxacin to block hERG channels (Alexandrou et al., 2006)."
38035013
reach
"Both moxifloxacin and dolasetron inhibit hERG and are known to cause QT prolongation and torsades des pointes and are labeled as drugs with proarrhythmic liability."
29879475
reach
"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