Table 1.
IC50 values for RuR and Ru360
| Inhibitor | Construct | EC50 (μM) | n | |
|---|---|---|---|---|
| RuR | K2P2.1 (TREK-1) | K2p2.1 (TREK-1) | >100 | 3 |
| K2p2.1 I110D | 0.287 ± 0.054 | 3 | ||
| K2p2.1 I110E | 13.6 ± 2.7 | 3 | ||
| K2p2.1 I110K | >100 | |||
| K2p2.1 I110D/G137I | 0.154 ± 0.023 | 3 | ||
| K2p2.1 I110D + 50 μM ML335 |
0.173 ± 0.021 | 3 | ||
| K2p2.1 N147D | 47.7 ± 6.3** | 2 | ||
| K2p2.1 N147E | 0.0733 ± 0.0165 | 3 | ||
| K2p2.1 I110D/N147D | 0.0127 ± 0.0023 | 3 | ||
| K2p2.1 I110D/N147E | 0.0126 ± 0.0034 | 3 | ||
| Other K2Ps | K2p10.1 (TREK-2) [D135]* | 0.23 ± 0.06 μM (Braun et al., 2015) | ||
| K2p9.1 (TASK-3) [E70]* | 0.114 ± 0.021 μM | 3 | ||
| Ru360 | K2P2.1 (TREK-1) | K2p2.1 (TREK-1) | >100 | 3 |
| K2p2.1 I110D | 11.3 ± 1.8 | 3 | ||
| Other K2Ps | K2p10.1 (TREK-2) [D135]* | 2.8 ± 1.2 | 3 | |
| K2p9.1 (TASK-3) [E70]* | 15.6 ± 2.7 | 3 | ||
n number of oocytes
Errors are SEM.
‘*’
residue at the K2P2.1 (TREK-1) I110D equivalent position
**
Lower bound constrained to 0.2