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. Author manuscript; available in PMC: 2014 Jul 25.
Published in final edited form as: Bioorg Med Chem. 2012 Jul 3;20(17):5269–5276. doi: 10.1016/j.bmc.2012.06.042

Table 1.

VGSC affinity, functional blockade, and acute toxicity15

Compound % [3H] BTX-B
displacement
(40 µM)		 % Nav1.2
functional block
(10 µM)		 Acute toxicity
(i.p.) LD50 (mg/kg)
DPH 28 11±4
[139–178]		 15615
Compound 1 70 31 ±5
[55–175]		 93
Compound 2 86 59 ±4
[646–2650]		 2000

% BTX displacement: In vitro displacement of [3H] BTX-B by DPH, 1, and 2 in rat forebrain membranes. Compounds were applied at 40 µm. % Navl.2 block was measured in vitro in HEK cells expressing Nav 1.2 compounds were applied at 10 µM. Compound toxicity was calculated using the OECD up-and-down test guideline 425 (LD50). Values are statistical estimates based on the long-term fate of 7–10 mice per dose. Beneath the LD50 values are 95% confidence intervals where the assumed sigma is 0.5 mg/kg. The DPH acute toxicity data was previously published.