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Cisapride inhibits KCNH2. 62 / 73
1 5 5 | 1 61
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"Other reports have indicated that residues F656 and Y652 cooperate in the binding of MK-499 [13,22] ; indeed, the hydrophobic surface area of F656 and the aromaticity of Y652 appear to be required for[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
16616004
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"On the other hand, the application of 1 μM cisapride completely abolished the tail current of hERG ( Fig. 4 (B), n = 3), indicating that cisapride blocked the potassium current of hERG."
20736054
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"In addition to the Phase-I compounds evaluated as part of the CiPA initiative we sought to assess the effect of additional well known hERG channel inhibitors such as cisapride and dofetilide side by s[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
27282640
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"Using this technique it was discovered that cisapride potently and selectively inhibited hERG (IC 50 s ranging from approximately 6–50 nM depending upon the protocol used) via binding to the open and/[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
23538024
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"The positive control, Cisapride, inhibited hERG current at 90 nM by 87.6%."
37872357
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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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"Blockage of the HERG human cardiac K+ channel by the gastrointestinal prokinetic agent cisapride."
9374794
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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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"Dofetilide and cisapride acutely inhibit hERG current."
26543354
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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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"PIX did not influence the action potential duration with an IC50 > 60 μM (Fig. S12I), while cisapride blocked (positive control) the hERG channel with an IC50 of 14.3 nM (Fig. S12H)."
36318018
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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
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"Structurally related EAG channels were made sensitive to the hERG blocker cisapride by moving the Tyr residue by one position along the S6 helix [ 31 ]."
15718164
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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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"Conversely, the positive control, cisapride (n = 4), inhibited hERG channel current at the 3, 10, 50, and 200 nM concentrations (Table 1); the estimated half maximal inhibitory concentration (IC ) for cisapride on hERG was 11.5 nM (Hill coefficient = 1.0)."
39980062
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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
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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
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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
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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
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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
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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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"These values are similar to those observed for the inhibition of HERG by cisapride under identical experimental conditions."
9395068
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"These results suggest that cisapride blocks an activated state of HERG, possibly the open state."
9395068
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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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"Dofetilide, cisapride, sotalol, terfenadine and verapamil blocked hERG channels at 37degreesC with an IC50 of 7nM, 18nM, 343muM, 165nM and 214nM, respectively."
30561737
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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
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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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"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
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"The rates of hERG current inhibition by 0.4 µM cisapride and by simnotrelvir at different concentrations were calculated with the peak tail current recorded for the negative control set to 100%."
37833261
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"Dynamic, pulse-by-pulse variation in the extent of observed I hERG inhibition by cisapride could be exacerbated by reducing the duration of the shorter depolarising step from 500 ms to 100 ms and by v[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
20172036
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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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"Furthermore, cisapride block of the HERG K+ current was not linked with inactivation in the mutant HERG channels F656V and F656M."
15967876
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"Several known hERG blockers, including dofetilide, terfenadine, cisapride, and E-4031, inhibit recombinant hERG currents in our hERG stable cell line and I Kr current in cardiac myocytes with the same[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
17596950
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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
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"Moreover, in the presence of hERG blockers such as cisapride (formerly used as a prokinetic agent), smooth muscle segmental contractions increased."
18329284
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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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"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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"Cisapride inhibited hERG channels transfected into CHO-K1 cells with pIC 50 of 7.8 ( Walker et al., 1999 )."
24769304
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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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"In a kidney cell line expressing the hERG channel, cisapride dose-dependently inhibited the hERG current [44]."
22985444
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"27 hERG blockers such as terfenadine ( 3 ), cisapride ( 4 ), and MK-499 ( 5 ) contain characteristic basic amine and hydrophobic groups ( Fig. 3 ), and the docking mode of these compounds in the hERG [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
26071372
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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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"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 presence of LPC-233 did not result in substantial hERG ion channel current inhibition (< 5% inhibition) at tested concentrations (0.3, 1, 3, and 10 μM), whereas the positive control compound cisapride inhibited hERG channel (69 ± 4 % inhibition) at 0.05 μM (Table S6)."
37556556
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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
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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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"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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"We tested the hypothesis that cisapride blocks HERG."
9374794
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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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"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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"Blockage of the HERG human cardiac K+ channel by the gastrointestinal prokinetic agent cisapride."
20408739
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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
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"In this experiment, HEK293 cells stably expressing the hERG protein were studied, and it was found that cisapride dose-dependently inhibited the hERG current with an IC of 32.63 ± 3.71 nM (Figure 1B), and a high dose (1,000 nM) caused 100% inhibition of the hERG current (Figure 1A)."
35935820
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"When the hERG current was thoroughly inhibited by 1 μM cisapride alone, no EAD/DAD/VT/VF occurred spontaneously or was induced."
35935820
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"Exposure to the prokinetic 5-HT receptor agonist and hERG blocker cisapride resulted in a pronounced reduction in ABR and VBR, agreeing with the known suppression of cardiac output by 5-HT receptor ag[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
24140389
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"When hERG currents were completely inhibited by cisapride 1 μM alone, the AP increased without significant changes in dispersion, and no spontaneous or induced EAD/DAD/VT/VF occurred."
35935820
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"In this context, the results obtained in our study are not surprising, since the KCNT1 antagonists herein reported do not present basic nitrogens (CPK16 and CPK20) or their nitrogens have low pK values (CPK4, CPK13, and CPK18—Jaguar predicted pK values: 4.48, 5.76, and 5.28, respectively) compared to the nitrogens of hERG blockers such as quinidine, astemizole, cisapride, and dofetilide."
38782404
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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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"Cisapride at a concentration of 10 microM completely blocked the hERG channels."
| PMC
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"When paced at 1.2 Hz (Figure 3(b)), the effect of L-673 on beating rate was masked until 3000 nM (at which concentration, cells had a faster spontaneous beating rate than 1.2 Hz), but effects on impedance amplitude and FPD (no correction, as rate was a constant under pacing condition, Figure 3(b) were similar to those without external stimulation.Because L-673 had shown effects on FPDcF beginning at 1 nM concentration, we co-applied L-673 (0.1, 0.3 and 1 nM) with the specific hERG blocker cisapride at 3, 10 and 30 nM concentrations that do not cause early afterdepolarizations (EADs) alone in hiPSC-CMs to avoid measurement interference."
31217965
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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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"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."
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