Table 4.
Mean current block at the highest drug concentrations tested in experiments (Chigh).
| Drug | Chigh | × Cmax | ICaL (%) | IK1 (%) | IKs (%) | INa (%) | INaL (%) | Ito (%) |
|---|---|---|---|---|---|---|---|---|
| Dofetilide | 6 nM | 3 | 1.2 | 3.4 | 0.2 | 2.5 | 4.6 | 27.0 |
| Bepridil | 3 uM | 90.9 | 50.7 | 0.5 | 16.2 | 51.7 | 67.0 | 2.4 |
| Sotalol | 2100 uM | 143.0 | 26.0 | 38.6 | 30.6 | 3.9 | 11.0 | 11.4 |
| Quinidine | 5.4 uM | 1.7 | 20.2 | 5.6 | 55.5 | 22.3 | 31.8 | 64.2 |
| Cisapride | 125 nM | 48.1 | 0.7 | 5.3 | 1.8 | 2.4 | 0.0 | 13.2 |
| Terfenadine | 800 nM | 200 | 52.0 | 0.0 | 3.3 | 14.0 | 12.7 | 20.6 |
| Ondansetron | 20 uM | 143.9 | 47.4 | 3.0 | 9.9 | 25.5 | 51.6 | 2.0 |
| Chlorpromazine | 10.5 uM | 276.3 | 55.4 | 51.1 | 5.2 | 84.2 | 69.2 | 6.0 |
| Verapamil | 1 uM | 12.3 | 85.7 | 3.9 | – | 0.5 | 12.0 | 9.9 |
| 500 nM | 6.2 | – | – | 2.4 | – | – | – | |
| Ranolazine | 23 uM | 11.8 | 2.5 | 0.3 | 2.1 | 17.4 | 72.3 | – |
| 69 uM | 35.4 | – | – | – | – | – | 26.5 | |
| Mexiletine | 10 uM | 2.4 | 19.5 | 0.6 | 0.0 | 6.1 | 51.9 | 1.0 |
| Diltiazem | 12.5 uM | 102.5 | 97.0 | 4.6 | 0.0 | 17.7 | 40.6 | 11.0 |
Concentrations are also expressed as multiples of the maximum therapeutic concentration (× Cmax). Because some ionic current experiments used different test concentrations, verapamil and ranolazine both have two entries in the table.