Inhibition of veratridine-induced delayed inactivation of the voltage-sensitive sodium channel by synthetic analogs of crambescin B.

  title={Inhibition of veratridine-induced delayed inactivation of the voltage-sensitive sodium channel by synthetic analogs of crambescin B.},
  author={Tadaaki Tsukamoto and Yukie Chiba and Atsuo Nakazaki and Yuki Ishikawa and Yoshiki Nakane and Yuko Cho and Mari Yotsu-Yamashita and Toshio Nishikawa and Minoru Wakamori and Keiichi Konoki},
  journal={Bioorganic \& medicinal chemistry letters},
  volume={27 5},
Crambescin B carboxylic acid, a synthetic analog of crambescin B, was recently found to inhibit the voltage-sensitive sodium channels (VSSC) in a cell-based assay using neuroblastoma Neuro 2A cells. In the present study, whole-cell patch-clamp recordings were conducted with three heterologously expressed VSSC subtypes, Nav1.2, Nav1.6 and Nav1.7, in a human embryonic kidney cell line HEK293T to further characterize the inhibition of VSSC by crambescin B carboxylic acid. Contrary to the previous… 
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