IndraLab

Statements

Cisapride inhibits KCNH2. 64 / 64
5 18 | 1 40
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"These values are similar to those observed for the inhibition of HERG by cisapride under identical experimental conditions."
9395068
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"The high-affinity intra-cavity blockade of hERG1 by cisapride depends on the hydrogen bonds formed by the pore-helix and on stabilizing aromatic interactions with residues in the S5 and S6 helices."
24606761
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"Under voltage-clamp conditions, cisapride block of HERG is dose dependent with a half-maximal inhibitory concentration of 6.5 nM at 22 degrees C (n = 25 cells)."
9374794
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"While cisapride inhibited potently the hERG channel currents, tegaserod failed to affect platelet aggregation, and had only a small contractile effect on the canine coronary artery at high concentrations."
23201772
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"The observation that cisapride block of hERG loses its dependence upon the extent of inactivation when F656 is mutated, or when internal K + was substituted for Cs +, has added to this model to suggest that inactivation gating reconfigures the position of F656 to one that is conducive to high affinity binding of cisapride, and that the internal permeant ion influences this repositioning 38."
29563525
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"Cisapride dose-dependently inhibited the hERG current with a half inhibitory concentration (IC50) of 32.63 ± 3.71 nM."
35935820
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"The postulated mechanism for this anti-proliferative effect is down-regulation of Cyclin D1, delaying progression through the cell cycle XREF_BIBR similar to what was observed with the hERG blocker cisapride XREF_BIBR."
20625512
ctd
No evidence text available
30561737
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"Cisapride inhibited the HERG channels in a concentration dependent manner with an IC (50) of 2.4 10 (-7) M."
11714889
tas
No evidence text available
12747773
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"Cisapride, a drug removed from the market because it caused long QT (LQT) syndrome and torsade de pointes (TdP), was used to induce hERG inhibition."
35935820
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"Block of cardiac hERG K + channels by the antihistamine terfenadine and the prokinetic agent cisapride is associated with prolonged ventricular repolarization and an increased risk of ventricular arrhythmia."
18987434
tas
No evidence text available
26761776
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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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"Our results suggest that inactivation facilitates cisapride block of HERG channels through affecting the positioning of Phe 656."
15967876
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"In the present study, we examined the effect of inactivation gating on cisapride block of HERG."
15967876
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"At -20 mV, 10 nM cisapride reduced HERG tail-current amplitude by 5%, whereas, at + 20 mV, the tail-current amplitude was reduced by 45% (n = 4 cells)."
9374794
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"As with dofetilide, HERG inhibition by cisapride required channel activation, which implies a predominant affinity for open and inactivated states of the HERG channel (Walker et al., 1999)."
11430924
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"Dofetilide and cisapride acutely inhibit hERG current."
26543354
ctd
No evidence text available
11741928
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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."
25625756
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"The effects of drugs on the trafficking of other cardiac ion channel proteins are largely unknown, but cisapride can cause QT prolongation by rescuing an abnormal misprocessed sodium channel protein called SCN5A and inhibiting hERG block (Liu et al., 2005) ."
35148401
tas
No evidence text available
15911273
ctd
No evidence text available
11005845
tas
No evidence text available
19534531
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"Cisapride at 6.3 muM reduced WT hERG channel currents by 80%, but only reduced S624A current by approximately 50% and Y652A current by approximately 15% (XREF_FIG)."
18987434
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"In this study, HERG block by quinidine and cisapride was assessed in extracellular solutions of calcium, potassium, rubidium, cesium and tetraethylammonium (TEA) using two-electrode voltage clamping of Xenopus oocytes."
19617705
ctd
No evidence text available
24052561
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"At this concentration, cisapride completely inhibited the WT hERG current, while inhibiting only about 20% or less of the currents from the mutants."
33004839
ctd
No evidence text available
24830940
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"We tested the hypothesis that cisapride blocks HERG."
9374794
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"We found that although inactivation facilitated cisapride block of the HERG K+ current, it was not coupled with cisapride block of HERG when the Cs+ current was recorded."
15967876
ctd
No evidence text available
14975710
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"The concentrations of cisapride needed to block HERG in the present study are likely to be encountered under certain clinical settings."
9395068
ctd
No evidence text available
27553911
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"Furthermore, cisapride block of the HERG K+ current was not linked with inactivation in the mutant HERG channels F656V and F656M."
15967876
ctd
No evidence text available
14678746
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"One example of the latter has been documented by Di Diego et al XREF_BIBR who showed that cisapride (a potent blocker of HERG channel) induced transmural dispersion of repolarization and torsade de pointes in the canine left ventricular wedge preparation during epicardial stimulation."
24475014
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"The only compound that triggered EADs was hERG blocker Cisapride."
22353256
ctd
No evidence text available
15272206
ctd
No evidence text available
12388285
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"Finally, the IC 50 value for cisapride block of HERG under these conditions measured 6.70 nmol/l."
9395068
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"2 In a chronic transfection model using CHO-K1 cells, cisapride inhibited HERG tail currents after a step to +25 mV with similar potency at room and physiological temperatures (IC50 16."
10510456
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"These results suggest that cisapride blocks an activated state of HERG, possibly the open state."
9395068
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"Blockage of the HERG human cardiac K+ channel by the gastrointestinal prokinetic agent cisapride."
9374794
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"These properties are compared with four known HERG channel blockers including verapamil, cisapride, ketoconazole and dofetilide in the XREF_TABLE."
23313619
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"Several other potent hERG channel blockers, such as astemizole and cisapride, were later reported to rescue the trafficking of LQT2 associated hERG channels harboring the G601S mutation."
24747662
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
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"These results demonstrate that at lower extracellular potassium concentrations, the permeant ion is almost exclusively responsible for the reduction in quinidine and cisapride block of HERG due to increases in extracellular potassium."
19617705
ctd
No evidence text available
12052668
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"XREF_BIBR Metoclopramide is also an antagonist at D 2 dopamine receptors and at 5-HT 3 receptors, while cisapride blocks 5-HT 2 and 5-HT 3 receptors and the human ether-a-go-go-related gene (hERG)-encoded K + channel."
22356640
ctd
No evidence text available
22198052
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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."
30561737
ctd
No evidence text available
15671647
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"Using patch clamp electrophysiology, we found that cisapride was a potent inhibitor of HERG displaying an IC50 value of 44.5 nmol/l when tail currents at -40 mV were measured following a 2 s test depolarization to +20 mV."
9395068
ctd
No evidence text available
9395068
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"Terfenadine (n = 459 cells) and cisapride (n = 83 cells) elicited 81.7 +/- 7.0% and 83.4 +/- 7.7% (mean +/- SD) hERG current inhibition, with 96-97% of data within 2 standard deviations of the mean."
32221320
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"Specifically, the KIC values were in agreement with the values reported for the L-type Ca 2+ channel blocker verapamil, the L-type Ca 2+ channel activator Bay K 8644, the K ATP channel opener levcromakalim, the hERG K + channel activator NS1463 and the hERG blockers cisapride and E-4031."
22926323
tas
No evidence text available
21185626
ctd
No evidence text available
15740727
ctd
No evidence text available
28551711
ctd
No evidence text available
17513944
ctd
No evidence text available
15306208
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"Cisapride at a concentration of 10 microM completely blocked the hERG channels."
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