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Domperidone inhibits KCNH2. 7 / 11
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"Recently, we also confirmed the modulating role of P-gp on the HERG-blocking properties of domperidone, a well-characterized I Kr -blocker [44] and P-gp substrate [35] ."
19233195
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"Initial study showing that domperidone prolonged the action potential duration in guinea-pig hearts and inhibited hERG current in Chinese Hamster Ovary cells.37."
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"With our model, Domperidone was predicted to block hERG potassium channels and possess a moderately high binding affinity of IC50=0.17μM. Ebastine is a H1 receptor antagonist used in the treatment of allergic rhinitis and chronic idiopathic urticaria."
36599209
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"In reporting APD prolongation and hERG block by domperidone for the first time, Drolet et al. quoted mean plasma concentrations of domperidone in humans of ~ 18 -- 21 ng/ml (42 -- 49 nM) at a dose of 30 mg/day [36]."
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"Domperidone is a medication used to treat nausea and vomiting often caused by other drugs to treat disease like Parkinson’s. Domperidone can block the hERG ion channel and is labeled a medication with intermediate risk to cause fatal arrhythmias.5 19 We tested the effect of domperidone on atrial hiPSC-CMs by measuring intracellular calcium flux response to clinically relevant doses (Figures S8F–S8J)."
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"Both domperidone and metoclopramide concentration-dependently blocked HERG currents, and the following values were calculated for IC (50) (the concentrations causing half-maximal inhibition) and n (the Hill coefficient) : 57.0 nmol/l and 0.99 for domperidone, 5.4 micromol/l and 0.95 for metoclopramide."
15640612
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"Domperidone has been studied in experiments on hERG expressing Chinese Hamster Ovary cells; in these, hERG current (IhERG) was inhibited by domperidone in a concentration dependent manner, with inhibition observed with 12 nM, and an estimated half-maximal inhibitory concentration (IC50) of 162 nM [36]."
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