Table 1. Summary of IC50 values and hill coefficients (nH) determined from concentration-response relationships for all studied blockers.
Name | WT |
Y652A-hERG |
F557L-hERG |
|||||
---|---|---|---|---|---|---|---|---|
IC50 (μM) | nH | IC50(μM)/% block @100 μM | nH | ∆IC50 | IC50(μM)/% block @100 μM | nH | ∆IC50 | |
Dofetilide | 2.5 ± 0.2 n = 4 | 1.3 ± 0.2 | 23% n = 5 | 0.6 ± 0.2 | >50 | 31% n = 7 | 0.5 ± 0.4 | >50 |
Terfenadine | 1.1 ± 0.04 n = 6 | 2 ± 0.2 | 9.3 ± 2.3 n = 4 | 1.03 ± 0.2 | 8.4 | 12.8 ± 2.3 n = 8 | 1.3 ± 0.1 | 11.6 |
Astemizole | 0.25 ± 0.02 n = 6 | 1.1 ± 0.1 | 4.4 ± 0.3 n = 5 | 0.9 ± 0.1 | 17.6 | 1.6 ± 0.2 n = 6 | 1.1 ± 0.1 | 6.4 |
Cisapride | 1.1 ± 0.1 n = 5 | 0.9 ± 0.03 | 81.4 ± 8.1 n = 4 | 1.03 ± 0.1 | 74 | 10.1 ± 0.6 n = 7 | 0.7 ± 0.03 | 9.2 |
Haloperidol | 1.3 ± 0.1 n = 4 | 1.3 ± 0.1 | 40.1 ± 1.9 n = 4 | 1 ± 0.04 | 31.4 | 30.3 ± 7.5 n = 4 | 1.7 ± 0.3 | 23.3 |
Amiodarone | 2.7 ± 0.3 n = 5 | 2.1 ± 0.4 | 13.5 ± 1.05 n = 5 | 2.3 ± 0.2 | 5 | 9.02 ± 1.05 n = 5 | 3.1 ± 0.2 | 3.34 |
(n = number of experiments).