TABLE 2.
Pharmacology of KCa2.3 and KCa3.1 point-mutated channels
Numbers in a parentheses indicate the number of independent experiments. For information on the pharmacological properties of additional KCa2.3/KCa3.1 chimeras, see Supplemental Table 1.
| Mutants | NS8593 IC50 | Current Inhibition by 100 μM BMB | TRAM-34 IC50 |
|---|---|---|---|
| μM | % | μM | |
| KCa2.3 WT | 0.104 ± 0.034 (13) | 83 ± 13 (10) | >20a |
| KCa2.3S507T | 2.5 ± 0.78 (9) | 42 ± 18 (5) | >>1 (3) |
| KCa2.3A532V | 3.1 ± 1.3 (4) | 67 ± 12 (2) | 2.7 (1) |
| KCa2.3S507T + A532V | >10 (3) | 65 ± 15 (3) | 0.064 ± 0.068 (2) |
| KCa3.1 WT | >10 (11) | 0 ± 0 (5) | 0.004 ± 0.002 (4) |
| KCa3.1T250S | 0.503 ± 0.209 (11) | 0 ± 0 (5) | 22 ± 14 (2) |
| KCa3.1V275A | 3.5 ± 1.6 (14) | 0 ± 0 (7) | 21 ± 4.3 (3) |
| KCa3.1T250S + V275A | 0.056 ± 0.024 (3) | 1 ± 1 (2) | >20a |