Table 1. Effects of P-CTX-1 on NaV channel voltage dependence of activation and steady-state fast inactivation.
P-CTX-1 | Maximal Peak Current (I/Imax) | Activation |
Inactivation |
|||
---|---|---|---|---|---|---|
V1/2 (mV) | k (mV) | V1/2 (mV) | k (mV) | |||
NaV1.1 | — | 0.99 ± 0.00 | −20.2 ± 0.4 | 4.5 ± 0.3 | −51.8 ± 1.2 | −6.7 ± 1.1 |
+ | 0.95 ± 0.04 | −25.3 ± 0.7* | 4.7 ± 0.6 | −53.8 ± 1.3 | −6.9 ± 1.2 | |
NaV1.2 | — | 1.00 ± 0.00 | −20.6 ± 0.3 | 4.4 ± 0.3 | −53.4 ± 0.6 | −4.1 ± 0.5 |
+ | 0.86 ± 0.09 | −26.9 ± 0.8* | 4.9 ± 0.7 | −60.3 ± 1.2* | −5.6 ± 1.1* | |
NaV1.3 | — | 1.00 ± 0.00 | −19.7 ± 0.3 | 4.9 ± 0.2 | −58.0 ± 0.5 | −4.1 ± 0.5 |
+ | 1.08 ± 0.04 | −24.7 ± 0.3* | 3.9 ± 0.2* | −60.1 ± 0.6* | −4.2 ± 0.7 | |
NaV1.4 | — | 0.93 ± 0.04 | −36.8 ± 0.4 | 1.8 ± 0.3 | −63.8 ± 0.5 | −4.6 ± 0.4 |
+ | 0.74 ± 0.16 | −40.2 ± 0.8* | 2.8 ± 0.7 | −57.3 ± 1.5* | −5.8 ± 1.4 | |
NaV1.5 | — | 0.93 ± 0.03 | −37.6 ± 1.0 | 4.6 ± 0.9 | −72.3 ± 0.6 | −5.8 ± 0.6 |
+ | 0.85 ± 0.07 | −43.7 ± 1.3* | 4.8 ± 1.1 | −72.8 ± 0.8 | −6.2 ± 0.7 | |
NaV1.6 | — | 1.00 ± 0.00 | −19.2 ± 0.2 | 4.8 ± 0.2 | −56.0 ± 0.4 | −5.1 ± 0.3 |
+ | 1.11 ± 0.03* | −22.6 ± 0.2* | 3.5 ± 0.2* | −57.1 ± 0.9 | −5.4 ± 0.8 | |
NaV1.7 | — | 0.91 ± 0.02 | −33.2 ± 0.6 | 3.2 ± 0.5 | −62.4 ± 0.4 | −4.4 ± 0.4 |
+ | 0.74 ± 0.10 | −38.9 ± 1.5* | 6.4 ± 1.4* | −64.4 ± 0.9 | −5.7 ± 0.8 | |
NaV1.8 | — | 0.94 ± 0.02 | −5.6 ± 0.6 | 7.7 ± 0.6 | −35.3 ± 1.7 | −8.7 ± 1.5 |
+ | 1.00 ± 0.08 | −16.9 ± 0.3* | 4.0 ± 0.2* | −36.1 ± 1.7 | −7.9 ± 1.5 | |
NaV1.9 | — | 0.99 ± 0.01 | −48.3 ± 0.7 | 7.8 ± 0.6 | −31.1 ± 2.1 | −11.4 ± 1.6 |
+ | 1.06 ± 0.15 | −57.2 ± 1.1* | 8.4 ± 1.0 | −41.7 ± 2.6* | −12.7 ± 2.2 |
Electrophysiological parameters at hNaV1.1–hNaV1.9 heterologously expressed in HEK293 cells were assessed using whole-cell voltage-clamp recordings. Data are reported as mean ± SEM from 4–10 cells. *Indicates P < 0.05 compared to control.