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Sotalol inhibits KCNH2. 26 / 36
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"The IC for hERG block by sotalol were measured by fitting the data to Hill’s equation as follows: f(D)=11+(D/IC50)h where f(D) is the current ratio in the presence of the drug at a given concentration (D) and h is the Hill coefficient.The data and datasets generated and analyzed in the current study can be accessed upon request sent to the corresponding author of the manuscript.3."
34062207
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"Blockade of the HERG ( I Kr ) channel by the class III anti-arrhythmic agents E4031 and sotalol prolonged QT in hPSC-CMs, as predicted."
22269465
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"The expected response to these drugs was seen only in iPS-CMs in which IKr was pharmacologically blocked with hERG blockers sotalol or dofetilide or reduced due to genetic defect in KCNH2 in an iPSC based model of LQTS-2 [99]."
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"Thus, we concluded that human iPSC-CMs can recapitulate cardiotoxicity and identify the effects of well-characterized compounds.Previous studies have demonstrated that sotalol, chlorpromazine, and mexiletine inhibit hERG currents, which may explain the cardiac toxicity of these drugs [14-16]."
37078300
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"This study investigated hERG block by cisapride , dofetilide , terfenadine , sotalol , and E-4031 - positive controls commonly used to demonstrate assay sensitivity - using the manual whole cell patch clamp method and an action potential-like voltage protocol presented at 0.2 Hz ."
35792285
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"The IC50 for hERG block by sotalol were measured by fitting the data to Hill 's equation as follows : ."
34062207
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"To analyse the rate-dependency of this effect, we tested the beta-blocker Sotalol that is known to also inhibit hERG channels and prolong the QT duration in patients 45."
28851973
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"Torsadogenic hERG blockers such as sotalol and quinidine produced statistically and physiologically significant effects, consistent with patch-clamp studies on human embryonic stem cell derived cardiomyocytes (hESC-CMs)."
24030418
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"As expected, hERG channel inhibitors such as sotalol, dofetilide, quinidine, and ranolazine caused a dose-related FPD prolongation independently from their classifications, confirming findings reported in previous studies (Blinova et al., 2017; Kanda et al., 2018; Millard et al., 2018)."
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"Dofetilide, cisapride, sotalol, terfenadine and verapamil blocked hERG channels at 37degreesC with an IC50 of 7nM, 18nM, 343muM, 165nM and 214nM, respectively."
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"This analysis shows that enhancements of endogenous HF oscillations in HR were also found in beagle dogs with dofetilide and with other hERG blockers such as cisapride, haloperidol, risperidone, DL sotalol, terfenadine and thioridazine."
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"It should be mentioned that cisapride, dofetilide, and sotalol directly inhibit hERG channel activity whereas quinidine decreases the surface expression of hERG channels by suppressing hERG channel translocation to cell membrane surface XREF_BIBR."
28102360
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"How to resolve disconnect between clinical and experimental data One of the longstanding conundrums related to hERG block by sotalol is that relatively high concentration of drug required to block the channel when assessed in isolated cloned channels expressed in vitro compared to the relatively low plasma concentrations reported in humans that apparently result in substantial QT interval prolongation [ 34,82,115 ] ."
34062207
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"First, we investigated the beta-blocker Sotalol, which is known to block also hERG K + channels and thereby induce a pharmacological Long QT syndrome with the high risk of arrhythmia [XREF_BIBR, XREF_BIBR]."
29211031
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"This study also reported that some classical hERG blockers, including atenolol, terfenadine, and sotalol, did not exhibit facilitation [43]."
38003453
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"We found at physiological temperature, that 150 μM sotalol inhibited hERG current 42.0 ± 3.2% (n = 4, IC 50 = 151 μM)."
22406079
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"Fig. 5 C shows an example of the use of a step-ramp protocol to assess I hERG inhibition by the low potency inhibitor sotalol (followed by application of a supramaximal concentration of cisapride to [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
18616963
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"Surprisingly, some classical hERG channel blockers like sotalol and ibutilide failed to prolong QTc interval in SQT1-patients, suggesting that the mutation in the hERG channel changed the sensitivity of the channel to drugs."
34025432
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"Experimental data suggest that Y652 in the S6 segment plays important roles in the ability of sotalol to block hERG, but unlike high-affinity sulfonamide blockers, sotalol binding is not affected by SF residue S624 mutations."
38035013
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"We found at physiological temperature, that 150 μM sotalol inhibited hERG current 42.0 ± 3.2% (n = 4, IC 50 = 151 μM)."
22406079
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"Sotalol blocked A-935142 enhanced hERG current 43.5 ± 1.5% (measurement made relative to peak of enhanced current), similar to the amount of hERG current block elicited by sotalol alone (p = 0.193 sot[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"These data show that sotalol blockade of A-935142 enhanced hERG current remains concentration dependent.In order to determine if our results were only applicable to sotalol, we repeated these combinat[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"The N588K mutation has been shown to significantly attenuate sotalol induced blockade of hERG channels, while attenuating that of quinidine to a lesser extent.This is concordant with previous data showing that the molecular determinants of hERG blockade for some low affinity blockers (e.g., [89]) may differ from those associated with class III antiarrhythmic agents [45,50]."
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"Similarly, a good correlation between individual susceptibility and drug-induced QT prolongation of moxifloxacin and the hERG blocker sotalol has been recapitulated (Shinozawa et al., 2017; Stillitano et al., 2017)."
35433691
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"They showed that torsadogenic hERG blockers, such as sotalol and quinidine, induced early afterdepolarization and ectopic beats in iPSC cardiomyocytes with a significantly higher rate than untreated controls (Navarrete et al. 2013)."
| PMC
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"Amiodarone, azimilide, dofetilide, quinidine and sotalol all produced a dose dependent inhibition of HERG current."
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