Ciguatoxin and brevetoxins share a common receptor site on the neuronal voltage-dependent Na+ channel

FEBS Lett. 1987 Jul 27;219(2):355-9. doi: 10.1016/0014-5793(87)80252-1.

Abstract

Binding studies indicate that ciguatoxin and brevetoxin allosterically enhance in a very similar way the binding of [3H]batrachotoxinin A 20-alpha-benzoate to the neuronal Na+ channel protein. Moreover ciguatoxin competitively inhibits the binding of [3H]brevetoxin-3 to rat brain membranes. The affinity of ciguatoxin for the Na+ channel is at least 20-50-times higher than that of brevetoxin. These results indicate that ciguatoxin and brevetoxins act at the same binding site on the sodium channel.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Brain / metabolism*
  • Ciguatoxins / pharmacology*
  • Ion Channels / drug effects
  • Ion Channels / metabolism*
  • Kinetics
  • Marine Toxins / pharmacology*
  • Neurons / metabolism*
  • Neurotoxins / metabolism
  • Oxocins*
  • Rats
  • Receptors, Cholinergic / drug effects
  • Receptors, Cholinergic / metabolism*
  • Sodium / metabolism*

Substances

  • Ion Channels
  • Marine Toxins
  • Neurotoxins
  • Oxocins
  • Receptors, Cholinergic
  • Ciguatoxins
  • brevetoxin
  • Sodium