Table 1.
The IC50 concentration or the maximum concentrations of compounds (1–12) against Nav1.1–Nav1.7
| Compound | Nav1.1 | Nav1.2 | Nav1.3 | Nav1.4 | Nav1.5 | Nav1.6 | Nav1.7 |
|---|---|---|---|---|---|---|---|
| TTX (1) | 4.1 ± 0.2 nM (n = 4) | 14 ± 2 nM (n = 3) | 5.3 ± 0.6 nM (n = 5) | 7.6 ± 2.6 nM (n = 3) | 1.0 ± 0.1 μM (n = 3) | 2.3 ± 0.0 nM (n = 3) | 36 ± 7 nM (n = 5) |
| CHTX (2) | 26 ± 1 nM (n = 5) | 27 ± 7 nM (n = 3) | 14 ± 2 nM (n = 7) | 50 ± 3 nM (n = 3) | 1.9 ± 0.9 μM (n = 4) | 43 ± 10 nM (n = 4) | 471 ± 27 nM (n = 7) |
| 8‐deoxyTTX (3) | 4.8 ± 0.46 μM (n = 3) | >300 nM | 4.9 ± 0.4 μM (n = 3) | 5.1 ± 1.4 μM (n = 3) | >300 nM | 4.6 ± 0.2 μM (n = 3) | >300 nM |
| 4,9‐anhydro‐TTX (4) | ND | ND | ND | >100 nM | >100 nM | 294 ± 25 nM (n = 3) | ND |
| 4,9‐anhydro‐CHTX (5) | ND | ND | ND | >100 nM | >100 nM | ND | ND |
| 4,9‐anhydro‐8‐deoxyTTX (6) | ND | ND | ND | >100 nM | >100 nM | ND | ND |
| 5‐deoxyTTX (7) | 57 ± 6 μM (n = 3) | >300 nM | 12 ± 1 μM (n = 3) | 4.5 ± 1.0 μM (n = 3) | >300 nM | >300 nM | >300 nM |
| 5,11‐dideoxyTTX (8) | >300 nM | >300 nM | >300 nM | >300 nM | >300 nM | >300 nM | >300 nM |
| 5,6,11‐trideoxyTTX (9) | >300 nM | >300 nM | >300 nM | >300 nM | >300 nM | >300 nM | >300 nM |
| 4,9‐anhydro‐5‐deoxyTTX (10) | ND | ND | ND | >100 nM | >100 nM | ND | ND |
| 4,9‐anhydro‐5,11‐dideoxyTTX (11) | ND | ND | ND | >100 nM | >100 nM | ND | ND |
| 4,9‐anhydro‐5,6,11‐trideoxyTTX (12) | ND | ND | ND | >100 nM | >100 nM | ND | ND |
The IC50 concentrations for TTX (1), CHTX (2), 8‐deoxyTTX (3) and 5‐deoxyTTX (7) are presented as the means ± SEM. The number of experiments is indicated in parentheses below the IC50 values. VSSC subtypes that were not tested for inhibitory activity of the test compound are marked as ND.