IndraLab

Statements

KCNH2 inhibits potassium(1+). 13 / 13
| 12 1
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"At 10 µM, aconitine, 14-benzoylaconine 8- O-palmitate, songoramine, gigactonine and neolinine demonstrated significant hERG K+ channel inhibition; all other compounds exerted only low (6-21%) inhibitory activity."
20862641
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"Lowering the extracellular potassium concentration ([K +] o) decreases the magnitude of I Kr and of outward HERG K + currents."
12356854
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"Furthermore, potassium channels were inhibited by 25D-NBOMe treatment in hERG assay."
30658151
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"HERG1 channel subunit composition mediates proton inhibition of rapid delayed rectifier potassium current (IKr) in cardiomyocytes derived from hiPSCs."
36496073
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"Cardiac toxicity was based on the hERG model, which predicts whether the compound blocks the hERG K+ channel or not."
29954088
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"39, 40 Indeed, the duration of phase 2 of the action potential is prolonged through hydroxychloroquine inhibition of the hERG channels, slowing the potassium rapid inward currents (iKr), and by means of sodium current enhancement exerted by azithromycin on SC5NA."
| PMC
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"These results demonstrate that hypoxia enhances the production of ROS in the mitochondria, resulting in down-regulation of hERG translation and decreased hERG mediated K+ conductance."
18570888
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"Pharmacokinetic properties, druglikeness as well as other significant descriptors, such as molecular weight, H-bond donors, H-bond acceptors, solvent accessible surface area, log HERG (blockage of K+ channels), log S (aqueous solubility), log P (octanol and water), and human oral absorption, for the selected hits were determined by QikProp (XREF_TABLE)."
25937949
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"CMX-2043 produced no inhibition of hERG mediated potassium current at its limit of solubility (3000muM; 1220mug/mL) when assessed using whole-cell patch-clamp electrophysiological methods."
24751172
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"The mechanisms by which these three drugs inhibit potassium channels, hERG in particular, have been studied previously and involve direct block of the pore via the intracellular vestibule and are coordinated by aromatic side-chains, such as phenylalanine."
32408169
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"A Hodgkin-Huxley-style cardiac ionic model captured the different types of complex dynamics following blockage of the hERG mediated potassium current."
23020479
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"However, compared to other inward rectifiers which block potassium conductance via an intracellular polyamine block, HERG channels prevent potassium outflow by rapid inactivation."
22988442
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"Computer calculations were performed using pharmacokinetic and pharmacodynamic data, including affinity to block the rapid component of the delayed rectifier cardiac potassium current (I Kr) encoded by the human ether-a-go-go gene (hERG), propensity to prolong cardiac repolarization (QT interval) and cause torsade de pointes (TdP)."
32888379