Journal: ACS Chemical Biology
Article Title: Na v 1.1 Modulation by a Novel Triazole Compound Attenuates Epileptic Seizures in Rodents
doi: 10.1021/cb500108p
Figure Lengend Snippet: Effect of 100 μM
rufinamide on human Na v channel
isoforms involved in epilepsy. (A) Molecular organization of rufinamide
consisting of the 1,2,3-triazole ring connecting the 2,6-difluorophenyl
and the carboxamide. (B–E) The left column shows G / G max and I / I max relationships, whereas the right column
displays the recovery from fast inactivation. The figure shows that
rufinamide inhibits hNa v 1.1 opening whereas the effect
on hNa v 1.6 is not significant compared to the effect of
DMSO treatment of this particular isoform (see Table ). Furthermore, the recovery from fast inactivation slows
for the four Na v channel isoforms tested here. All data
are shown before (green, DMSO control) and after (red) addition of
100 μM rufinamide to hNa v 1.1 (B), hNa v 1.2 (C), hNa v 1.3 (D), and hNa v 1.6 (E). All
fit values are listed in Table . n = 5–8, and error bars represent the standard error of the
mean.
Article Snippet: Human (h) hNa v 1.1 (NM_001165963.1), hNa v 1.2 (NM_021007.2), hNa v 1.3 (NM_006922.3), hNa v 1.6 (NM_014191.3), and hβ 1 (NM_001037.4) clones were obtained from OriGene Technologies, Inc., and modified with an ER forwarding motif and the rNa v 1.2a 3′UTR region for expression in Xenopus laevis oocytes (acquired from Xenopus One).
Techniques: