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. 2008 Oct 27;75(2):281–295. doi: 10.1124/mol.108.051425

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).