IndraLab

Statements

KCNH2 inhibits pyraclofos. 8 / 8
| 8
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"In SQT1, a gain-of-function mutation in KCNH2 impairs the voltage dependent inactivation of I Kr."
26425105
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"In the micromolar concentration range NS309 blocks hERG channels (IC 50 = 1.3 muM) and CyPPA blocks voltage gated sodium channels (IC 50 = 11 muM), whereas NS13001 had no effect on these channels at concentrations as high as 10 muM (data not shown)."
23102227
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"Kcnh2 is a voltage-activated potassium channel that hyperpolarizes the plasma membrane by conducting K out of the cell, thereby maintaining keratinocytes.87 Kcnj8 channels are inwardly rectified K channels that maintain membrane potential depolarization.88 Interestingly, Kcnj8 activation and Kcnh2 inhibition promote wound healing and facilitate the net inflow of potassium into cells."
39600531
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"The results of our study can be summarized as follows : 1) acepromazine inhibited the hERG channels in a concentration dependent manner; 2) the drug also blocked hERG channels voltage dependently between -40 mV and +60 mV; 3) acepromazine inhibited the hERG currents by acting on both the inactivated (during the depolarization) and open (during the repolarization) states of the channels; 4) the result of fast drug application study was consistent with the open-channel block mechanism of hERG channel by acepromazine."
28066143
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"I kinetics data for the truncated construct, hERG , are limited to date, showing a modest (+5 mV) shift in voltage‐dependent activation, whilst the channel retained sensitivity to inhibition by the high affinity inhibitors dofetilide and astemizole (Wang & MacKinnon, 2017)."
33091232
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"HERG1 expression within the nucleus reduced hERG1 current density by depolarizing the voltage dependence of activation and stabilizing inactivation."
36626562
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"Gating current studies suggest that a slow component of hERG gating charge, Q on, underlies S4 voltage sensor movement with a time constant of ~ 50 ms at +10 mV which is slightly faster than channel activation, and a V (1/2) that is about 20 mV hyperpolarized compared to the conductance-voltage (G-V) relationship in both WT and S631A inactivation removed channels XREF_BIBR."
20526358
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"Therefore, S631 mutations that disrupted C-type inactivation also facilitated hERG channel activation in the negative voltage range."
10354437