Table 2 Percent current inhibition of WT and mutant hERG channels by various compounds.
hERG WT | hERG Y652A | hERG F656A | ||
|---|---|---|---|---|
Compound | Concentration (µM) | |||
Cisapride | 1 | 98.60% ± 1.40 | 7.70% ± 0.69 | 18.78% ± 5.69 |
3 | 99.41% ± 0.59 | 39.10% ± 2.27 | 38.66% ± 8.08 | |
5 | 99.89% ± 0.11 | 57.70% ± 3.91 | 59.61% ± 7.46 | |
10 | 100.00% ± 0.00 | 91.72% ± 5.64 | 75.51% ± 13.26 | |
Mosapride | 1 | 13.07% ± 3.47 | 7.13% ± 3.47 | 10.99% ± 1.77 |
3 | 33.48% ± 2.66 | 13.58% ± 2.28 | 12.45% ± 0.29 | |
5 | 44.96% ± 1.27 | 20.57% ± 3.01 | 16.03% ± 8.18 | |
10 | 68.74% ± 1.83 | 31.30 ± 3.65 | 25.71% ± 5.72 | |
30 | 92.45% ± 7.55 | 66.85% ± 12.66 | 34.35% ± 3.53 | |
100 | 40.21% ± 5.60 | |||
Ranolazine | 10 | 42.27% ± 2.12 | 2.40% ± 0.76 | 4.39% ± 0.24 |
30 | 76.97% ± 2.85 | 10.13% ± 0.48 | 10.86% ± 5.72 | |
100 | 97.36% ± 0.89 | 24.62% ± 2.64 | 21.37% ± 7.80 | |
300 | 100.00% ± 0.00 | 64.00% ± 6.08 | 37.74% ± 11.09 | |
500 | 100.00% ± 0.00 | 84.56% ± 4.88 | 49.62% ± 8.87 | |
Lidocaine | 10 | 2.99% ± 1.19 | 3.03% ± 1.77 | 5.49% ± 2.75 |
30 | 7.79% ± 1.00 | 5.53% ± 2.52 | 8.10% ± 3.59 | |
100 | 19.13% ± 1.75 | 11.94% ± 0.64 | 15.08% ± 1.78 | |
300 | 42.21% ± 4.03 | 25.66% ± 0.54 | 26.63% ± 3.49 | |
500 | 56.06% ± 3.55 | 45.01% ± 2.90 | 35.48% ± 5.19 | |
n = | 3 | 3 | 2 to 6 |
