Table 2. Summary of BL-1249 Analogue Activation of K2P2.1(TREK-1) and K2P4.1(TRAAK)a.
| compound | K2P2.1(TREK-1) EC50 (μM) | n (≥) | K2P4.1(TRAAK) EC50 (μM) | n (≥) |
|---|---|---|---|---|
| BL-1249 | 5.5 ± 1.2 | 3 | 48 ± 10b | 3 |
| BL-1249-amide | 22 ± 8 | 3 | >200 | 3 |
| BL-1249-acid | 44 ± 10c | 4 | >200 | 2 |
| BL-1249-Ph | >200 | 3 | >200 | 3 |
| BL-1249-tricycle | 34 ± 6 | 2 | 42 ± 9 | 3 |
a
Data derived from at least two independent experiments with each data point averaged from at least three oocytes.
b
EC50 estimated imposing an upper boundary of 15 (fold activation, I/I0).
c
EC50 estimated imposing an upper boundary of 20 (fold activation, I/I0)