TABLE 1

Results of screening benzothiazoles varied in positions 1 and 2 on KCa2.3 and KCa3.1 at concentrations of 1, 10, and 100 μM

The reported numbers are the ratios of slope conductance at −80 mV measured in the presence and absence of drug with 250 nM [Ca2+]i.

Compound
Name
KCa2.3
KCa3.1
1 μM
10 μM
100 μM
1 μM
10 μM
100 μM
1 Riluzole Embedded Image 1.1 ± 0.3 11.5 ± 4 30 ± 3 6 ± 1 30 ± 1.5 30 ± 2
2 SKA-12 Embedded Image N.E. 1.5 ± 0.2 3.9 ± 1.2 N.E. 2.1 ± 1.4 34 ± 9
3 SKA-5 Embedded Image N.E. N.E. N.D. N.E. N.E. 23 ± 5
4 SKA-6 Embedded Image N.E. N.E. N.D. N.E. 2.0 ± 1.0 15 ± 4.0
5 SKA-46 Embedded Image N.E. 1.8 ± 0.1 17 ± 1.5 N.E. 2.9 ± 1.0 30 ± 8
6 SKA-47 Embedded Image N.E. 2.3 ± 0.5 8.4 ± 3.5 N.E. 2.0 ± 1.0 25 ± 12
7
SKA-41
Embedded Image
N.E.
1.7 ± 0.4
32 ± 5
N.E.
N.E.
1.3 ± 0.5

  • N.E., no effect; N.D., not determined.