IndraLab

Statements

Erythromycin A inhibits KCNH2. 19 / 25
2 3 | 13 6
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"The results of this study document that both erythromycin and clarithromycin significantly inhibit the HERG potassium current at clinically relevant concentrations."
14674677
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"A metabolite of erythromycin, des-methyl erythromycin, was also found to inhibit HERG current with an IC (50) of 147.1 microM."
12065733
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"[Erythromycin inhibits the proliferation of HERG K+ channel highly expressing cancer cells and shows synergy with anticancer drugs]."
17313833
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"XREF_BIBR - XREF_BIBR, XREF_BIBR, XREF_BIBR Similar to AZA1 (C 47 H 71 NO 12), the macrolide antibiotic erythromycin (C 37 H 67 NO 13) also blocks hERG1 rapidly in an open-state dependent manner and analysis of mutant channels and molecular modeling indicate that it interacts with phenylalanine reside at position 656 but not with tyrosine reside at position 652."
22856456
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"It is noteworthy that the hERG blocker erythromycin blocks cell cycle in G2 phase if administered together with vincristine."
21850047
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"Erythromycin has been shown to block hERG channels at physiological temperature with an IC 50 of approximately 40muM."
22131976
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"At a concentration of 100muM, erythromycin causes no significant block of hERG currents at RT but significantly blocks currents at physiological temperature."
22131976
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"The same was true for other hERG channel blockers (like erythromycin, moxifloxacin and sematilide) and multi-ion channel blockers."
29311989
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"At higher concentrations (300muM), erythromycin did block hERG currents at RT by approximately 40% and gave an IC 50 of 427.5 muM calculated from the graph (n = 12)."
22131976
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"At 300muM, erythromycin blocked hERG currents at 35degreesC by 70% and the IC 50 at this temperature was calculated to be 30.7 muM (n = 18)."
22131976
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"Understanding how erythromycin inhibits the hERG could help us to decide which compounds are needed for further studies."
37446837
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"Temperature-Dependent Inhibition of hERG by Erythromycin."
37446837
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"The IC 50 at RT is approximately 11-fold higher than that at PT, suggesting that erythromycin inhibits the hERG current not only in a concentration-dependent manner but also in a temperature-dependent manner."
37446837
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"The reversal of hERG inhibition by erythromycin could be unique."
37446837
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"Compounds with strong APD prolonging ability include Ca 2+ channel agonists like Bay K8644; class Ia antiarrhythmics (e.g., quinidine); unintended hERG channel blockers like the antibiotic erythromycin; certain class III antiarrhythmics (e.g., E4031); and a large variety of neurotoxins (e.g., anemone toxin)."
30210937
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"Figure xref shows the concentration dependence of I hERG inhibition by erythromycin, terfenadine and thioridazine under the recording conditions of this study, with representative traces of effects of single drug concentrations shown in Figure xref i–ci and concentration–response relations shown in Figure xref ii–cii."
32147975
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"Pretreatment with erythromycin induced an approximately 14-22-fold reduction in hERG affinity for pore binding drugs at concentrations of erythromycin, which by themselves only block hERG by 10% or less."
24417241
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"Mean data comparing percentage of I hERG tail inhibition by 600 µM erythromycin is shown in Figure xref ."
32147975
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"XREF_BIBR Hyperthermia exaggerates block of HERG by erythromycin in LTC cells as well as APD prolongation by this drug in mouse isolated ventricular myocytes."
19649147