TABLE 4.
Pharmacological properties of sMamb-1 variants
IC50 values (mean ± S.E.) of the inhibition of rat ASIC1a current by wild-type and sMamb-1 variants. Asterisks indicate a statistically significant difference compared with wild-type sMamb-1 (Kruskal-Wallis test followed by a Dunn's post hoc test done from 4–10 dose-response curves for each mutant). Note that two-electrode voltage clamp recordings have been obtained using a manual setup, leading to an IC50 value for sMamb-1 that is not exactly the same as the one obtained with the Roboocyte2 automated workstation shown in Fig. 3A (10 versus 3.4 nm, respectively).
| Peptide | IC50 | Hill slope | -Fold change |
|---|---|---|---|
| nm | |||
| sMamb-1 | 10 ± 1 | 1.1 ± 0.1 | - |
| H21A | 31 ± 3 | 1.4 ± 0.2 | 3.1 |
| T23A | 39 ± 5 | 1.2 ± 0.1 | 3.8 |
| F27A | 341 ± 29*** | 1.3 ± 0.1 | 33.3 |
| R28A | 193 ± 11** | 1.2 ± 0.1 | 18.8 |
| N29A | 28 ± 2 | 1.2 ± 0.1 | 2.8 |
| L30A | 51 ± 3 | 1.1 ± 0.1 | 4.8 |
| K31A | 49 ± 2 | 1.4 ± 0.1 | 4.8 |
| L32A | 21979 ± 4174*** | 0.8 ± 0.1 | 2147.8 |
| I33A | 163 ± 5*** | 1.5 ± 0.1 | 15.9 |
| L34A | 579 ± 59*** | 1.3 ± 0.1 | 56.6 |
| K57A | 15 ± 4 | 1.2 ± 0.1 | 1.5 |