Table 1.

Changes in IC₅₀, k_on, and k_off for TTX with mutations in the outer vestibule (modified from Penzotti et al. [51]).

Mutation	Equilibrium IC50(μM)	kon (M−1s−1)	koff (s−1)	IC50 ratio
Native Nav1.4	0.036 ± 0.006	3.53 × 105	1.02 × 10−2.	1
D400A	6.0 ± 0.7	2.93 × 102	1.26 × 10−2	168
E403Q	161 ± 14	2.48 × 102	1.57 × 10−2	4521
E755A	229 ± 21	2.90 × 102	2.69 × 10−2	6412
E758Q	6.2 ± 0.3	4.86 × 103	1.47 × 10−2	174
K1237A	23 ± 2	1.62 × 102	1.49 × 10−2	641
M1240E	87 ± 5	4.15 × 102	1.98 × 10−2	2433
M1240K	238 ± 17	1.02 × 102	1.58 × 10−2	6678
D1532N	1.5 ± 0.2	6.14 × 102	1.45 × 10−2	43