IndraLab

Statements

KCNH2 inhibits pyraclofos. 7 / 7
| 7
reach
"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
reach
"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
reach
"In SQT1, a gain-of-function mutation in KCNH2 impairs the voltage dependent inactivation of I Kr."
26425105
reach
"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
reach
"In experimental systems varying from Drosophila to primary mammalian and human cell lines, celecoxib inhibits many voltage activated Na (+), Ca (2+), and K (+) channels, including NaV1.5, L- and T-type Ca (2+) channels, KV1.5, KV2.1, KV4.3, KV7.1, KV11.1 (hERG), while stimulating other K (+) channels-KV7.2 -5 and, possibly, KV11.1 (hERG) channels under certain conditions."
24630832
reach
"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
reach
"Therefore, S631 mutations that disrupted C-type inactivation also facilitated hERG channel activation in the negative voltage range."
10354437