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. Author manuscript; available in PMC: 2018 Jun 1.

Published in final edited form as: Epilepsia. 2017 Apr 27;58(6):1073–1084. doi: 10.1111/epi.13764

Table 3.

Comparison of Mouse and Rat 6 Hz Pharmacology for ASDs Acting on Na⁺ Channels

Compound	ED₅₀ and PI
	Mechanism of Action	Mouse Stimulus Intensity		Rat Stimulus Intensity
	Mechanism of Action	1.5×CC₉₇ (32mA)	2×CC₉₇ (44mA)	1.5×CC₉₇	2×CC₉₇
Carbamazepine	Blocks fast inactivation	23.7 (18.3–26.3) PI 1.9	38.2 (25.8–69.0) PI 1.2	>40 PI<0.9	>40 PI<0.9
Eslicarbazepine	Blocks fast inactivation	60.7 (46.1–72.4) PI 1.6	77.6 (61.3–92.4) PI 1.3	>200 PI n.c.	>200 PI n.c.
Lacosamide	Enhance slow inactivation	10.0 (7.7–12.8) PI 2.7	12.9 (9.8–18.2) PI 2.1	15.6 (6.3–30.0) PI 0.8	>50 PI<0.3
Lamotrigine	Blocks fast inactivation	19.5 (12.9–30.8) PI 1.5	43.4 (33.0–52.2) PI 0.7	>60 PI<0.4	>60 PI<0.4
Phenytoin	Blocks fast inactivation	37.5 (30.1–52.7) PI 1.3	44.6 (38.2–48.9) PI 1.1	30.7^a PI 0.5	>100 PI<0.2
Rufinamide	Enhance slow inactivation	23.1 (16.8–34.0) PI >2.0	32.9 (23.2–39.5) PI >1.4	42.7 (30.2–59.5) PI 8.2	n.c.^b

not calculated (n.c.); Protective Index (PI; TD₅₀/ED₅₀)

^a

95% CI exceeded the dose range tested

^b

Partial efficacy (50–65% efficacy) observed at doses of 80–200 mg/kg; reduced activity observed at a dose of 350 mg/kg

N=6–8 per group, 100–120g