IndraLab

Statements

Sotalol inhibits KCNH2. 21 / 21
5 | 3 12 1
ctd
No evidence text available
24052561
ctd
No evidence text available
22198052
reach
"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."
34062207
reach
"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
eidos
"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
reach
"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
ctd
No evidence text available
16757186
reach
"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."
25625756
reach
"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
ctd
No evidence text available
30561737
ctd
No evidence text available
16960444
sparser
"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
reach
"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
reach
"In whole-cell voltage clamp studies we found : 1) 60 muM A-935142 enhanced hERG current in the presence of 150 muM sotalol (57.5 +/-5.8%) to a similar extent as seen with A-935142 alone (55.6 +/-5.1%); 2) 150 muM sotalol blocked hERG current in the presence of 60 muM A-935142 (43.5 +/-1.5%) to a similar extent as that seen with sotalol alone (42.0 +/-3.2%) and 3) during co-application, hERG current enhancement was followed by current blockade."
22406079
reach
"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
reach
"Amiodarone, azimilide, dofetilide, quinidine and sotalol all produced a dose dependent inhibition of HERG current."
16960444
eidos
"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
eidos
"The IC50 for hERG block by sotalol were measured by fitting the data to Hill 's equation as follows : ."
34062207
reach
"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
reach
"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
reach
"Dofetilide, cisapride, sotalol, terfenadine and verapamil blocked hERG channels at 37degreesC with an IC50 of 7nM, 18nM, 343muM, 165nM and 214nM, respectively."
30561737