Comparison of activation effects (EC50 values) of fenamates on WT and A278R Slo2.1 channels
| Compounds | WT hSlo2.1 | A278R hSlo2.1 | Ratio (EC50-WT/EC50-A278R) | ||||
|---|---|---|---|---|---|---|---|
| EC50 | nH | n | EC50 | nH | n | ||
| mM | mM | ||||||
| Niflumic acid | 2.09 ± 0.14 | 2.4 ± 0.06 | 9 | 0.11 ± 0.01 | 2.0 ± 0.2 | 13 | 19 |
| Flufenamic acid | 1.1 ± 0.09 | 2.2 ± 0.16 | 5 | 0.059 ± 0.008 | 2.0 ± 0.1 | 6 | 19 |
| Mefenamic acid | 0.366 ± 0.03 | 1.5 ± 0.1 | 13 | 0.051 ± 0.006 | 1.7 ± 0.06 | 6 | 7.2 |
| Tolfenamic acid | 0.30 ± 0.02 | 1.9 ± 0.09 | 8 | 0.047 ± 0.004 | 2.0 ± 0.09 | 5 | 6.4 |
| Meclofenamic acid | 0.079 ± 0.006 | 1.7 ± 0.07 | 5 | 0.017 ± 0.005 | 1.7 ± 0.2 | 6 | 5 |
| Diclofenac | 0.72 ± 0.07 | 2.4 ± 0.2 | 5 | 0.31 ± 0.02 | 2.3 ± 0.16 | 5 | 2.3 |
| N-Phenylanthranilic acid | 0.79 ± 0.03 | 1.5 ± 0.03 | 7 | 0.29 ± 0.02 | 1.5 ± 0.06 | 8 | 3 |
| Diphenylamine | – | – | – | – | – | – | – |
| Anthranilic acid | – | – | – | – | – | – | – |
| N-Methylanthranilic acid | – | – | – | – | – | – | – |
| Biphenyl-2-Carboxylic acid | – | – | – | – | – | – | – |
| Benzyl-benzoic acid | – | – | – | – | – | – | – |
–, No activation.