Table 2. Effect of β-PMTX Analogs Across Sodium Channel Isoforms at 3.3 μMa.
|
AUC
ratio for
hNaV1.X activation at
3.3 μM |
|||||||
|---|---|---|---|---|---|---|---|
| Compounds | NaV1.1 | NaV1.2 | NaV1.3 | NaV1.4 | NaV1.5 | NaV1.6 | NaV1.7 |
| β-PMTX | 1.4 ± 0.05 | 0.9 ± 0.05 | 1.2 ± 0.1 | 0.8 ± 0.07 | 1.0 ± 0.1 | 1.3 ± 0.1 | 1.1 ± 0.06 |
| Peptide16 | 3.1 ± 0.3 | 1.8 ± 0.3 | 2.0 ± 0.3 | 1.4 ± 0.2 | 1.7 ± 0.5 | 3.1 ± 0.3 | 2.9 ± 0.3 |
| Peptide17 | 10.7 ± 1.7 | 2.4 ± 0.2 | 1.9 ± 0.1 | 1.6 ± 0.4 | 4.0 ± 1.3 | 6.7 ± 0.9 | 4.0 ± 0.3 |
| Peptide18 | 12.7 ± 1.2 | 7.1 ± 0.5 | 4.4 ± 1.6 | 1.6 ± 0.08 | 1.3 ± 0.04 | 8.1 ± 0.8 | 9.6 ± 0.5 |
a
The values represent the area under the curve (AUC) and its standard error. The AUC ratio was calculated as (peptide AUC/baseline AUC). For complete dose–response curves, see Supporting Information.