Table 3.
Inhibition by µ-SIIIA of cloned sodium channels expressed in Xenopus oocytes. Rate constants were determined as described under Experimental. Standard deviation and 95% confidence intervals (95% C.I) were calculated from at least three independent experiments using Prism software.
| Sodium channela |
kon (µM−1.min−1) |
koff (min−1) |
IC50(95% C.I.) (µM) |
|---|---|---|---|
| rNaV1.1 | 0.011 ± 0.004 | 0.2 ± 0.06 | 11 (9.3–12.6) |
| rNaV1.2 | 0.10 ± 0.015 | Irreversibleb | N.A.c |
| rNaV1.3 | 0.017 ± 0.002 | 0.12 ± 0.018 | 11 (9.0–12.9) |
| rNaV1.4 | 0.29 ± 0.036 | 0.04 ± 0.008 | 0.13 (0.11–0.16) |
| rNaV1.5 | --d | --d | 251 (204–308)e |
| mNaV1.6 | 0.06 ± 0.012 | 0.082 ± 0.006 | 0.76 (0.69–0.85) |
| rNaV1.7 | 0.005 ± 0.0005 | 0.075 ± 0.012 | 65 (57.8–73.1) |
α-Subunit cloned from rat (r) or mouse (m).
Although the block was essentially irreversible within the experimental time frame, the koff was estimated as 0.0047 ± 0.0015 min−1 based on residual recovery after 20 min of wash and assuming exponential decay.
Not available because slow kinetics precluded steady state from being achieved within the experimental time frame.
Unable to be determined because block was too small and apparent kinetics too fast to be measured accurately.
Extrapolated value assuming 100% block at saturating peptide concentration.