Table 1.
Experimental data for propafenone and derivatives
| Compound | IC50 (µM) | Concentration (µM) | Time constant of block (s) | Recovery after 330 s (%) | Time constant of recovery (s) |
|---|---|---|---|---|---|
| Propafenone | 3.79 ± 0.240 | 10 | 0.44 ± 0.110 | 05.43 ± 12.240 | – |
| GPV005 | 1.34 ± 0.04* | 4 | 0.66 ± 0.11* | 05.68 ± 10.010 | – |
| GPV009 | 0.84 ± 0.08* | 3 | 1.39 ± 0.14* | 01.67 ± 07.220 | – |
| GPV019 | 1.42 ± 0.18* | 4 | 1.82 ± 0.14* | 59.00 ± 02.77* | 72.31 ± 16.53 |
| GPV031 | 1.46 ± 0.19* | 4 | 1.65 ± 0.18* | 69.25 ± 07.62* | 97.60 ± 27.25 |
| GPV062 | 1.05 ± 0.05* | 3 | 2.15 ± 0.27* | 46.41 ± 02.35* | 44.59 ± 16.51 |
| GPV180 | 1.78 ± 0.15* | 5 | 0.87 ± 0.15* | 00.58 ± 09.130 | – |
| GPV574 | 5.04 ± 0.540 | 15 | 0.48 ± 0.090 | 60.55 ± 11.98* | 61.09 ± 46.05 |
| GPV576 | 1.84 ± 0.24* | 6 | 1.58 ± 0.17* | 61.03 ± 06.91* | 84.74 ± 23.34 |
| GPV929 | 1.27 ± 0.05* | 4 | 1.00 ± 0.13* | 04.55 ± 05.200 | – |
| SCT-AS03 | 0.77 ± 0.11* | 2 | 2.39 ± 0.39* | 12.26 ± 04.290 | – |
Data are given as means ± SEM from at least three experiments. Drug concentrations (≈3·IC50) for studying onset of and recovery from HERG channel block were chosen to induce substantial and comparable current inhibition.
*
P < 0.05, significantly different from propafenone (unpaired Student's t-test).