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Pyraclofos inhibits KCNH2. 39 / 39
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"XREF_FIG and XREF_FIG illustrate that Ca 2+ is not a voltage dependent blocker of HERG currents."
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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."
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"Together, these results suggest that voltage dependent block of HERG results from gating dependent changes in the accessibility of Y652, a critical component of the drug binding site."
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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."
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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)."
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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."
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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]"
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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]."
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"The two intersecting straight lines shown inFigure 6c,d represent estimates of voltage-dependent hERG inactivation and recovery-from-inactivation rates that approach asymptotically the experimental rate plots at extremities."
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"Coexpression of R863X with wild-type HERG showed reduced current densities and accelerated voltage dependent inactivation of HERG channels."
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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 )."
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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."
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"Extracellular protons accelerate hERG channel deactivation by destabilizing voltage sensor relaxation."
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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."
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"The voltage dependent inhibition of the hERG currents by olanzapine increased steeply in the voltage range of channel activation."
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"HERG current was rapidly and reversibly suppressed by external acidosis in a voltage independent manner."
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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 ."
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"Voltage dependent blockade of HERG channels expressed in Xenopus oocytes by external Ca2+ and Mg2+."
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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."
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"We propose that the Q fast charge movement during activation accompanies transitions through early closed states of the hERG activation pathway, and that the weak voltage dependence of these transitions limits the overall activation rate of hERG channels."
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"Atazanavir has been reported not to alter voltage dependent activation or inactivation of wild-type (WT) hERG current (IhERG), but protocols to interrogate a requirement for channel opening were not applied (39)."
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"We interpret this to indicate that stabilization of the activated voltage sensor limits the return of hERG channels to rest."
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"5: Concentration-dependent voltage shifts induced by chloroquine and hydroxychloroquine on half-activating and half-inactivating potentials of hERG1 channels stably expressed in HEK293T cells, assessed with specific voltage-clamp protocols in automated patch-clamp experiments."
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"The two intersecting straight lines shown in Fig. 6 c,d represent estimates of voltage-dependent hERG inactivation and recovery-from-inactivation rates that approach asymptotically the experimental rate plots at extremities."
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"XREF_BIBR Concentration and voltage dependent inhibitions of the hERG channel by ASP A were further investigated."
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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."
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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."
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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)."
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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."
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"Both strychnine and brucine were shown to exhibit the voltage dependent inhibition of hERG channels."
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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."
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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+."
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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]."
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"3.2 Voltage dependent inhibition of HERG channels."
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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."
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"The voltage dependent inhibition of hERG currents by endoxifen increased steeply in the voltage range of channel activation."
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"Both strychnine and brucine were shown to exhibit the voltage-dependent inhibition of hERG channels ( xref )."
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"Together these findings indicate a critical role for Tyr 652 in voltage dependent block of HERG channels."
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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."
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