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Pyraclofos inhibits KCNH2. 49 / 49
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"XREF_FIG and XREF_FIG illustrate that Ca 2+ is not a voltage dependent blocker of HERG currents."
10102937
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"This voltage shift reduces hERG channel inactivation at efflux assay potentials, and will reduce the affinity of hERG blocking drugs that bind to inactivated states of the channel."
15475478
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"The voltage dependent inactivation of hERG channels with 135 mM K + in the pipette solution (bath solution containing 5 mM K +) was also evaluated using the standard triple pulse protocol (XREF_FIG) and also plotted in XREF_FIG (O, n = 4)."
16769794
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"Increasing [K + ] e produced a +10 mV shift in voltage‐dependent inactivation of WT I hERG and slowed inactivation time course, while lowering [K + ] e from 4 to 1 mmol/L produced little change in inactivation voltage dependence, but accelerated inactivation time course."
25318749
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"The data were fitted with equation xref to derive V 0.5 and k values for voltage‐dependent inactivation of I hERG ."
25318749
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"The voltage dependent inactivation of hERG K+ channels, however, can be well described by a two-state mechanism (Wang et al. 2011) and so is amenable to analysis using theREFER technique.In a two-state process the kinetics of the transitionsbetween the two states are proportional to the height of the energy barrier separating the two end states (G+ +), whereas the equilibrium of the reaction is proportional to the energy difference between the two end states (G0)."
25820318
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"The voltage-dependent inhibition of hERG by endoxifen increased steeply in the voltage range of channel activation from 21.8±2.2% at −30 mV to 39.9±1.1% at 0 mV ( n =8, P <0.05), indicating that this [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
25680947
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"Both strychnine and brucine were shown to exhibit the voltage dependent inhibition of hERG channels."
33867974
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"Voltage dependent blockade of HERG channels expressed in Xenopus oocytes by external Ca2+ and Mg2+."
9508824
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"We further evaluated the effect of HW-0168 on voltage dependent activation and inactivation of hERG current."
31481348
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"These results indicated that the voltage dependent inhibition of the hERG currents by endoxifen can be explained by an interaction between the charged form of the drug and the binding sites in the ele[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
25680947
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"Atazanavir has been reported not to alter voltage dependent activation or inactivation of wild-type (WT) hERG current (I hERG ), but protocols to interrogate a requirement for channel opening were not applied ( xref )."
34017865
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"These results suggest that while intracellular Mg 2+ causes some voltage dependent block of the h-erg channel, Mg ` block may not necessarily account for all of the observed rectification of the insta[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
8766823
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"In the current study, we found that the drug trazodone also showed conflicting results with respect to its voltage-dependent inhibition of I hERG ."
24412489
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"Coexpression of R863X with wild-type HERG showed reduced current densities and accelerated voltage dependent inactivation of HERG channels."
14714110
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"The voltage-dependent inactivation of the hERG channel is reflected in the steady-state inactivation of the channel."
36720353
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"In conclusion, the voltage sensor of the initial half is able to confer near normal voltage dependent properties to the assembled construct, and the functional properties of the pore domain leading to the characteristic voltage dependent inactivation of HERG are maintained in the co-assembled channels."
25818916
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"It would be interesting to compare the effects of different stimuli on both voltage-dependent activation and inactivation of TRPA1.While molecular determinants for voltage-dependent activation and inactivation can be different [37, 38, 43, 56], the outer mouth of the pore loop has been implicated in voltage-dependent inactivation of HERG K channels [21, 41, 59]."
24092046
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"Extracellular protons accelerate hERG channel deactivation by destabilizing voltage sensor relaxation."
30530765
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"Thus, mutations Y652A decreased potency by a factor of three and F656T caused a seven fold reduction in drug potency.We previously reported that voltage-dependent block of HERG channels by chloroquine[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
16423345
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"The voltage dependent inhibition of hERG current resulted in the activation curve to be shifted to a negative voltage after primaquine exposure in a dose dependent manner."
20512476
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"Both strychnine and brucine were shown to exhibit the voltage-dependent inhibition of hERG channels ( xref )."
33867974
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"HERG current was rapidly and reversibly suppressed by external acidosis in a voltage independent manner."
10652186
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"To determine whether the Ca 2+ effect is due to a rapid voltage dependent block of open HERG channels, the method of XREF_BIBR was modified to accommodate HERG inactivation behavior."
10102937
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"The two intersecting straight lines shown in xref c,d represent estimates of voltage-dependent hERG inactivation and recovery-from-inactivation rates that approach asymptotically the experimental rate plots at extremities."
34785211
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"Second, the voltage dependent inhibition of HERG channels has been observed for both compounds although it is more significant by tetra-n-octylammonium bromide than benzethonium chloride."
23313619
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"The effect of strychnine and brucine on the voltage-dependent inactivation of hERG channels was determined using the protocol in the inset of Fig.5 A . The peak tail currents that were recorded by a t[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
30282042
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"Mutations in this loop affect the rapid voltage dependent inactivation of the HERG K + channel that is critical for its normal function [13]."
12650941
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"XREF_BIBR Concentration and voltage dependent inhibitions of the hERG channel by ASP A were further investigated."
25378909
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"First, the voltage dependent inhibition of hERG channels was observed for the two compounds in the standard I V protocol."
30282042
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"These studies have also shown that hERG channel voltage-dependent inhibition occurs in different states."
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"3.2 Voltage dependent inhibition of HERG channels."
24846011
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"In addition, stabilization of the activated voltage sensor in the relaxed state has been shown to slow hERG channel closing (Tan et al., 2012; Goodchild et al., 2015; Thouta et al., 2017)."
30530765
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"However, similar changes in the voltage dependent profile for block of Y652F or Y652A HERG channels were observed with vesnarinone, a cardiotonic drug that is uncharged at physiological pH. Together, these results suggest that voltage dependent block of HERG results from gating dependent changes in the orientation of Y652, a critical component of the drug binding site, and not from a transmembrane field effect on a charged drug molecule."
12695533
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"Based on the data obtained from above three different types of I-V curves, tetra-n-octylammonium bromide exhibited a significant voltage dependent inhibition of HERG currents in all three experiments."
23313619
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"When quantified as the relative tail current for voltage ranging from −30 to −10 mV ( Fig. 2 C), the percentage block gradually increased (32.7 ± 4.0% of block at −30 mV, 43.4 ± 3.0% at −20 mV and 48.[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
30954564
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"Together these findings indicate a critical role for Tyr 652 in voltage dependent block of HERG channels."
11960982
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"It is possible therefore that other interventions that significantly reduce HERG’s normal voltage-dependent inactivation could contribute to APD and QT interval shortening."
15325285
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"Removing external divalents does not remove deactivation, eliminating the possibility that slow voltage dependent block by divalent cations causes HERG deactivation."
10102937
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"The voltage-dependent activation, inactivation and deactivation of hERG1 channels are depicted in Fig. 3 ."
19351523
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"The effect of strychnine and brucine on the voltage-dependent inactivation of hERG channels was determined using the protocol in the inset of Fig."
30282042
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"Using a ventricular action potential voltage clamp protocol, halofantrine and N-desbutylhalofantrine block of HERG current was greatest during phases 2 and 3 of the action potential waveform."
12176129
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"Previous studies by Sanchez-Chapula et al indicate that Tyr-652 has a critical role in the voltage-dependent block of hERG channels ( Sanchez-Chapula et al., 2002 )."
19903464
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"In our study, Y652A did not alter the voltage-dependent block of hERG channels, but the V 1/2 of the activation curve was shifted in the depolarizing direction with an increase in slope factor and the[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
19903464
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"First, the voltage dependent inhibition of hERG channels was observed for the two compounds in the standard I V protocol."
30282042
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"After reaching the peak, both I‐V curves quickly decreased at more positive potentials because of the voltage‐dependent KCNH2 channel inactivation."
31361068
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"Thus, neither a time dependent nor -independent voltage dependent block of open HERG channels can explain the effect of extracellular Ca 2+."
10102937
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"Voltage dependent inhibition of hERG currents has been reported as a common characteristic of open-channel blocking compounds such as dofetilide (Snyders and Chaudhary, 1996)."
14729380
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"The voltage dependent inhibition of the hERG currents by olanzapine increased steeply in the voltage range of channel activation."
26484507