Journal: Molecular Pharmacology
Article Title: Amiodarone irrecoverably impairs the function of human ether-a-go-go-related gene potassium channels
doi: 10.1016/j.molpha.2025.100094
Figure Lengend Snippet: Acute effects of AMIO and DEA on the currents of hERG channels heterologously expressed in H9c2 cells. (A) I hERG traces recorded from the same cell in the CTL condition and after acute bath application of 0.3 μ M or 10 μ M AMIO. (B) Concentration-response relationships of acute AMIO-induced I hERG inhibition. I hERG -Rel is plotted against AMIO concentrations, and data are fitted to the Hill equation. Summarized I hERG -Rel was from 4 to 6 cells for each concentration in 3 independent experiments. (C) I hERG during AMIO application and washout relative to the CTL current (I hERG -Rel) plotted against time (n = 4). (D) I hERG traces recorded from the same cell in the CTL condition and after acute bath application of 1 μ M and 10 μ M DEA. (E) Concentration-response relationships of acute DEA-induced I hERG inhibition. I hERG -Rel is plotted against DEA concentrations, and data are fitted to the Hill equation. Summarized I hERG -Rel was from 3 to 4 cells for each concentration. (F) I hERG during DEA application and washout relative to the CTL current (I hERG -Rel) plotted against time (n = 3). Data are presented as mean ± SD.
Article Snippet: H9c2 cells were obtained from American Type Culture Collection (Manassas, VA) and cultured in Dulbecco’s modified Eagle’s medium (Gibco) supplemented with 10% FBS. hERG cDNA with N-terminal deletion (Δ2–354), C-terminal truncation from position 1073 (ΔC–1073), as well as point mutations in the pore loop (S620T, S631A), and common drug binding aromatic residues Y652A and F656V were constructed using PCR as described previously.
Techniques: Concentration Assay, Inhibition
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