Table 1.

Tool compound results.

Compound name	Nav1.2 (μM)	Nav1.2 95% CI (μM)	Nav1.5 (μM)	Nav1.5 95% CI (μM)	Nav1.7 (μM)	Nav1.7 95% CI (μM)	State dependence*
Amitriptyline	0.56	0.33–0.79	0.82	0.71–0.94	1.25	1.08–1.43	9.6
Tetracaine	0.26	0.18–0.34	0.43	0.35–0.50	0.28	0.23–0.34	15.5
Vixotrigine	1.74	1.30–2.17	0.93	0.72–1.14	1.36	1.06–1.68	29.8
JNJ63955918	3.07	1.90–4.24	6.26	4.97–7.55	0.042	0.035–0.049	6.1
PF-05089771	0.17	0.087–0.25	10.1	8.58–11.6	0.035	0.030–0.040	42.9
Tetrodotoxin	0.019	0.016–0.021	3.08	2.45–3.71	0.033	0.028–0.037	4.0
Carbamazepine	139.4	115.3–163.4	37.1	26.7–47.5	52.6	40.0–65.3	39.9
Funapide	0.51	0.35–0.66	0.24	0.15–0.32	0.46	0.38–0.54	2.7
Mexiletine	28.8	19.2–38.5	21.0	15.6–26.5	13.0	9.1–16.9	9.2
Lacosamide	392.9	286.3–499.6	58.5	46.9–70.1	104.6	84.2–125.0	n.a.
Lamotrigine	72.4	60.9–83.9	20.6	14.7–26.6	32.8	23.5–42.0	24.3
MK-0759	1.50	0.91–2.10	1.61	1.28–1.93	2.05	1.56–2.54	18.8
Lidocaine	47.2	25.6–68.9	20.1	14.9–25.2	15.0	14.0–15.8	15.4
TC-N 1752	0.14	0.13–0.15	1.15	0.84–1.46	0.046	0.043–0.050	10.8
VX-150	Inactive	n.a	Inactive	n.a	Inactive	n.a	n.a

Nav1.x IC₅₀ values, Nav1.x IC₅₀ 95% confidence intervals (CI), and state dependence from 15 tool compounds with different potencies and working mechanisms. *State dependence is defined as the ratio of IC₅₀ values of Nav1.7 spiking HEK assay at TP1 at 4 mM K⁺ over TP10 IC₅₀ values at 8 mM K⁺ (Figure 2B).