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

TABLE 2.

Screening of 4, 5, and 6 position-substituted benzothiazoles on KCa2.3 and KCa3.1

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
KCa2.3
KCa3.1
1 μM 10 μM 100 μM 1 μM 10 μM 100 μM
1 Riluzole graphic file with name zmo002095770t02a.jpg 1.1 ± 0.3 11.5 ± 4 30 ± 3 6 ± 0.9 30 ± 1.5 30 ± 2
8 SKA-1 graphic file with name zmo002095770t02b.jpg N.E. 1.9 ± 0.3 N.D. 1.3 ± 0.2 3.1 ± 0.3 35 ± 4
9 SKA-36 graphic file with name zmo002095770t02c.jpg N.E. 1.2 ± 0.2 15.5 ± 2 N.E. 1.2 ± 0.2 17 ± 1
10 SKA-4 graphic file with name zmo002095770t02d.jpg N.E. 1.2 ± 0.3 N.D. N.E. 1.2 ± 0.1 1.3 ± 0.1
11 SKA-16 graphic file with name zmo002095770t02e.jpg N.E. N.E. N.E. N.E. 1.5 ± 0.3 1.1 ± 0.3
12 SKA-24 graphic file with name zmo002095770t02f.jpg N.E. N.E. N.E. N.E. 4.0 ± 0.5 13 ± 2
13 SKA-2 graphic file with name zmo002095770t02g.jpg N.E. 2.0 ± 0.3 N.D. N.E. 1.1 ± 0.1 5.1 ± 0.4
14 SKA-17 graphic file with name zmo002095770t02h.jpg N.E. 1.4 ± 0.2 2.1 ± 1.0 1.4 ± 0.3 1.3 ± 0.4 2.2 ± 0.3
15 SKA-13 graphic file with name zmo002095770t02i.jpg 1.8 ± 0.2 3.3 ± 0.5 36 ± 4 1.3 ± 0.3 5.0 ± 1.0 29 ± 5
16 SKA-7 graphic file with name zmo002095770t02j.jpg N.E. N.E. N.E. N.E. 1.5 ± 0.3 14 ± 2
17 SKA-32 graphic file with name zmo002095770t02k.jpg N.E. N.E. N.E. N.E. N.E. N.E.
18 SKA-22 graphic file with name zmo002095770t02l.jpg N.E. 1.4 ± 0.2 Insoluble N.E. 1.2 ± 0.3 Insoluble
19 SKA-48 graphic file with name zmo002095770t02m.jpg 1.9 ± 0.1 12 ± 4 39 ± 8 4.3 ± 0.8 40 ± 7 35 ± 8
20 SKA-18 graphic file with name zmo002095770t02n.jpg 1.8 ± 0.2 6.5 ± 0.5 42 ± 5 3.0 ± 0.5 32 ± 5 39 ± 5
21 SKA-42 graphic file with name zmo002095770t02o.jpg 1.5 ± 0.1 3.5 ± 1.5 35 ± 5 1.3 ± 0.5 2.8 ± 6 14 ± 2
22 SKA-3 graphic file with name zmo002095770t02p.jpg 2.2 ± 0.4 14 ± 3 32 ± 3 2.0 ± 0.5 38 ± 3 41 ± 3
23 SKA-8 graphic file with name zmo002095770t02q.jpg 1.1 ± 0.2 7.4 ± 0.5 32 ± 3 6.0 ± 0.7 38 ± 5 34 ± 6
24 SKA-35 graphic file with name zmo002095770t02r.jpg 1.6 ± 0.5 3.5 ± 1.0 24 ± 3 1.2 ± 0.5 5 ± 3 26 ± 4
25 SKA-51 graphic file with name zmo002095770t02s.jpg 2.2 ± 0.9 18 ± 3 N.D. 1.6 ± 0.5 35 ± 7 N.D.
26 SKA-34 graphic file with name zmo002095770t02t.jpg 1.4 ± 0.3 2.5 ± 0.5 33 ± 5 2.5 ± 0.5 13 ± 6 32 ± 2
27 SKA-19 graphic file with name zmo002095770t02u.jpg 1.5 ± 0.3 10 ± 1 30 ± 3 1.2 ± 0.2 12 ± 4 29 ± 4
28 SKA-11 graphic file with name zmo002095770t02v.jpg 2.3 ± 0.9 22 ± 4 30 ± 5 3.0 ± 2 10 ± 3 19 ± 5
29 SKA-53 graphic file with name zmo002095770t02w.jpg N.E. Insoluble Insoluble N.E. Insoluble Insoluble

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