Drug potency on inhibiting late Na + current is sensitive to gating modifier and current region where drug effects were measured.

Journal of Pharmacological and Toxicological Methods(2019)

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摘要
I pharmacology can be impacted by all experimental factors examined in this study. The effect of gating modifier and current region used to quantify drug inhibition alone led to 30× difference in half inhibitory concentration (IC) for ritonavir, demonstrating that substantial difference in drug inhibition can be produced. Drug potencies on inhibiting I derived from different patch clamp studies may thus not be generalizable. For I pharmacology to be useful for in silico modeling or interpreting drug-induced changes in cardiac action potentials or ECG, standardizing I experimental procedures including data analysis methods is necessary to minimize data variability.
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关键词
IC50,INaL,ECG,CiPA
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