TABLE 4.
Selectivity
| Channel | Riluzole IC50 | 10 μM SKA-20 | 25 μM SKA-31 |
|---|---|---|---|
| μM | |||
| KCa1.1 | Doubles current at 100 μM | N.E. | N.E. |
| Kv1.1 | 92 ± 7 | 12 ± 3% block | N.E. |
| Kv1.3 | 50 ± 5 | 12 ± 2% block | 20 ± 5% block |
| Kv1.5 | 95 ± 5 | 25 ± 3% block | 20 ± 5% block |
| Kv3.1 | 95 ± 5 | 35 ± 3% block | 30 ± 5% block |
| Kv3.2 | 100 ± 10 | 12 ± 5% block | 15 ± 3% block |
| Kv4.2 | 130 ± 10 | 10 ± 3% block | N.E. |
| Kv11.1 (HERG) | 50 ± 4 | N.D. | N.E. |
| K2P2.1 (TREK-1) | 110 ± 35* | N.E. | N.E. |
| Nav1.2 | 15 ± 3 | 14 ± 2 μM | 9 ± 5% block |
| Nav1.4 | 9 ± 2 | N.E. | 20 ± 5% block |
| Nav1.5 | 8 ± 2 | 30 ± 5% block | 40 ± 5% block |
| Cav1.2 | 30 ± 3 | N.E. | N.E. |
N.E., no effect; N.D., not determined.
EC50 (riluzole activates K2P2.1 currents).