Table 4.
Condition | Peak Current Density (pA/pF) b | Tau of Fast Inactivation (ms) c | V1/2 of Activation (mV) d | V1/2 of Steady-state Inactivation (mV) e | Long Term Inactivation (Depolarization Cycles 2–4) f | ||
---|---|---|---|---|---|---|---|
2 | 3 | 4 | |||||
DMSO | –55.39 ± 2.16 (10) | 1.17 ± 0.09 (7) | –20.04 ± 0.85 (10) | –58.58 ± 1.90 (5) | 0.89 ± 0.03 | 0.86 ± 0.03 | 0.85 ± 0.04 (6) |
12 | –18.30 ± 2.02 ** (10) | 1.30 ± 0.11 (7) | –20.40 ± 0.89 (10) | –57.59 ± 0.56 (6) | 0.88 ± 0.03 | 0.76 ± 0.03 * | 0.70 ± 0.04 * (7) |
19 | –79.63 ± 3.55 ** (8) | 1.12 ± 0.07 (7) | –22.49 ± 0.72 * (8) | –58.53 ± 1.69 (8) | 0.83 ± 0.02 | 0.73 ± 0.02 * | 0.73 ± 0.03 * (8) |
a Summary of the electrophysiological evaluation of 12 and 19. Results are expressed as the mean ± SEM. The number of independent experiments is shown in parentheses. Significance was determined via unpaired t-test compared with 0.1% DMSO. * p < 0.05; ** p < 0.005. b Peak current density, which describes the number of channels in a conductive (open) state, is a measure of the maximum influx of Na+ current (pA) into the cell normalized to membrane capacitance (pF) to control for variable cell sizes. c Tau of fast inactivation measures the decay phase of Na+ currents to characterize the time required for channels to transition from the conductive (open) state to a nonconductive state resulting from fast inactivation. d V1/2 of activation is a measure of the voltage at which half of available channels transition from the closed to the conductive (open) state. e V1/2 of steady-state inactivation is a measure of the voltage at which half of channels are available to transition into the conductive (open) state, while the other half are non-conductive due to steady-state (closed-state) inactivation. f Long-term (slow) inactivation is a type of inactivation induced by successive or prolonged depolarization cycles that causes collapse of the S5–S6 pore module of Nav channels resulting in a prolonged nonconductive inactivated state.