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985 results
  • Drug potency on inhibiting late Na+ current is sensitive to gating modifier and current region where drug effects were measured. [Journal Article]
  • JPJ Pharmacol Toxicol Methods 2019 Jun 27; :106605
  • Wu M, Tran PN, … Wu WW
  • CONCLUSIONS: INaL 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 (IC50) for ritonavir, demonstrating that substantial difference in drug inhibition can be produced. Drug potencies on inhibiting INaL derived from different patch clamp studies may thus not be generalizable. For INaL pharmacology to be useful for in silico modeling or interpreting drug-induced changes in cardiac action potentials or ECG, standardizing INaL experimental procedures including data analysis methods is necessary to minimize data variability.
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