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Loperamide inhibits KCNH2. 16 / 17
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"As hERG channel inactivation is not expected below this membrane voltage (also see Fig. 3 F), these results suggest that loperamide blocks hERG channels in the open and not inactivated state.Steady st[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"This indicates that hERG inhibition by N -desmethyl loperamide is less likely to be a significant contributor to clinical QT prolongation relative to loperamide."
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"These results show that loperamide blocks hERG channels in a voltage-dependent manner, and shifts the voltage-dependence of steady state hERG current activation and inactivation.To evaluate the effect[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"In ion-channel studies, loperamide inhibited hERG (I Kr ) , I Na, and I Ca currents with IC 50 values of 0.390 muM, 0.526 muM, and 4.091 muM, respectively (i.e., >1560x FTPC)."
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"Loperamide can inhibit hERG voltage-gated potassium (K + ) channels (Kv11.1), leading to the prolongation of repolarization, QTc interval prolongation, and increased risk of torsades de pointes."
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"The 50% inhibitory concentration for loperamide inhibition of hERG ionic tail currents was approximately 40 nmol/l."
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"Finally, N -desmethyl loperamide inhibited hERG channel currents with an IC 50 value of 245 nM (220–272 nM, 95% confidence limits, n = 5–7, Fig. 2 C, D)."
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"At supra-therapeutic blood levels, loperamide can block cardiac HERG K channels leading to potentially fatal arrhythmias (Eggleston et al., 2016; Kang et al., 2016; Vaughn et al., 2016)."
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"These data were fit with the Hill equation, giving an IC 50 of 54.1 nM and a Hill coefficient of 0.69.These results show that loperamide blocks hERG channels in a concentration-dependent manner."
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"The time constants of hERG current suppression (interpreted as hERG channel block hence τ block ) by loperamide were concentration-dependent ( Fig. 2 C, D)."
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"Plotting the ratio of I tail obtained in loperamide and control solutions against the preceding test voltage showed that loperamide suppressed hERG current in a voltage-dependent manner ( Fig. 3 D)."
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"Plotting I tail against the test voltages for all cells showed that loperamide suppressed hERG current in both the inward and outward directions."
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"Second, the degree of hERG current suppression by loperamide correlated with voltage-dependence of steady state hERG current activation, suggesting that the drug-channel interaction requires channel o[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"Together, these results support the interpretation that loperamide blocks hERG channels in the open state.The rate of hERG channel block by loperamide was determined from the decay of hERG current in [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"Our preclinical studies have confirmed that loperamide inhibits hERG-mediated I in HEK293 cells with an IC of 390 nM (based on nominal concentrations)."
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"In other published studies, loperamide was reported to inhibit hERG at lower IC values from 33 to 89 nM [39,40,41] under different study conditions and measurement protocols."
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