Brain levels of sEHI correlate with observed activity.

<p>The sEHI TUPS was administered at a single i.p. dose of 1/kg and seizures were induced at varying times using s.c. PTZ procedure (n = 8/time point). Following tonic hind limb extension and lethality, brains were rapidly excised and TUPS was quantified by LC-MS/MS. Protected animals (3 of 8 in each group) were sacrificed 30 min following PTZ treatment and are included on the left panel. (A) TUPS was well absorbed and blood and brain inhibitor levels reached well over in vitro IC₅₀ values within an hour and remained relatively stable over 8 h. (B) The efficacy of TUPS was significantly correlated with brain inhibitor levels (Spearman's Rho, 0.90, p = 0.037) All time points are significantly different from the vehicle treated animals (One Way ANOVA, p = 0.034).