IndraLab

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Fentanyl inhibits KCNH2. 8 / 9
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"Thus, in addition to a greater susceptibility due to the presence of hERG1b in the human heart, hERG channel block by fentanyl can be exacerbated by certain conditions such as hypoxia, hypokalemia, or alkalosis, which may increase the risk of fentanyl induced ventricular arrhythmias and sudden death."
32321735
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"35 Oxycodone and fentanyl reduce HERG current in vitro, XREF_BIBR, XREF_BIBR and as do cocaine and cocaine metabolites, XREF_BIBR, XREF_BIBR but none of these drugs affect the I Ks current."
21895724
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"Moreover, fentanyl, a synthetic potent opioid receptor agonist, was reported to block HERG channel currents in ventricular myocytes (Tschirhart et al., 2019)."
38707245
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"Based on the current literature, methadone, oliceridine, l-α-acetylmethadol (LAAM), and fentanyl were found to inhibit the HERG channel function and were associated with QTc prolongation."
37015297
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"When hERG tail currents upon -50 mV repolarization following a 50 mV depolarization were analyzed, fentanyl and naloxone blocked hERG current (I hERG) with an IC 50 of 0.9 muM and 74.3 muM, respectively, while norfentanyl did not block."
30665971
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"We have demonstrated that fentanyl blocks hERG current (I hERG) at concentrations that overlap with the upper range of postmortem blood concentrations in fentanyl related deaths."
32321735
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"When a voltage protocol that mimics a human ventricular action potential (AP) was used, fentanyl blocked I hERG with an IC 50 of 0.3 muM."
30665971
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"As well, high pH potentiated the fentanyl mediated block of hERG channels, with an IC 50 at pH 8.4 being 7-fold lower than that at pH 7.4."
32321735