TABLE 2

Characterization of activation of hNa_v1.7 mutants in the presence of 100 nM HWTX-IV

Cells were held at −100 mV. Families of currents were induced by 50-ms depolarizing steps to various potentials ranging from −80 to +40 mV. Recording currents from WT and mutant Na_v1.7 started at ∼20 min after establishing whole-cell configuration. All data come from three to four cells. The half-activation potential (V_1/2) and slope factor (k) were determined with Boltzmann fits. IC₅₀ values were determined with Hill equation in Fig. 2B, in which slope factor was set to 1. The f_bottom values yielded were 0 on both wild-type and mutant Na_v1.7 channels and therefore are not listed.

Channel	Voltage Dependence of Activation
	Control		HWTX-IV
	V_1/2	k	V_1/2	k	IC₅₀
	mV	mV	mV	mV	nM
hNa_v1.7	−38.8 ± 0.8	6.8 ± 0.7	−40.2 ± 0.7	7.3 ± 0.6	22.7 ± 6.3
L201V/N206D	−40.4 ± 1.3	7.9 ± 1.2	−36.7 ± 1.2	9.6 ± 1.1	20.8 ± 3.6
F813G	−32.7 ± 1.0	6.7 ± 0.9	−36.3 ± 1.4	8.0 ± 1.3	28.2 ± 5.7
E818C	−41.6 ± 0.8^{^a}	7.1 ± 0.7^{^a}	−39.7 ± 0.9^{^a}	8.9 ± 0.8^{^a}	9120.1 ± 1400.0
E203K/E818C	−20.5 ± 0.3^{^a}	8.5 ± 0.3^{^a}	−16.0 ± 1.1^{^a}	13.8 ± 1.0^{^a}	8892.0 ± 1135.2
F204A/F813G	−46.7 ± 0.4	4.5 ± 0.3	−42.7 ± 0.4	6.1 ± 0.3	26.7 ± 6.4

↵a The concentration of HWTX-IV was 10 μM.