The voltage-gated sodium ion channel inhibitory activities of a new tetrodotoxin analogue, 4,4a-anhydrotetrodotoxin, and three other analogues evaluated by colorimetric cell-based assay

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8 Citations (Scopus)

Abstract

The voltage-gated sodium ion channel inhibitory activities of four tetrodotoxin analogues were evaluated for their ability to reduce the cytotoxicity of ouabain and veratridine in mouse neuroblastoma Neuro-2a cells. EC 50 of the novel analogue, 4,4a-anhydrotetrodotoxin purified from pufferfish, was 750 fold larger than that of tetrodotoxin, supporting the implication of 4-OH in activity. The high activity of 11-oxotetrodotoxin was confirmed. Modification of C-6 of 11-nortetrodotoxin-6,6-diol to form an oxime derivative decreased the activity to 1/22.

Original languageEnglish
Pages (from-to)72-76
Number of pages5
JournalToxicon
Volume119
DOIs
Publication statusPublished - 2016 Sep 1

Keywords

  • 11-Oxotetrodotoxin
  • 4 4a-anhydrotetrodotoxin
  • Maleimide
  • Neuro-2a
  • Tetrodotoxin
  • Voltage-gated sodium ion channel

ASJC Scopus subject areas

  • Toxicology

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