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. 1974 Oct;71(10):3936–3940. doi: 10.1073/pnas.71.10.3936

Evidence That Tetrodotoxin and Saxitoxin Act at a Metal Cation Binding Site in the Sodium Channels of Nerve Membrane

R Henderson 1,2,3,*, J M Ritchie 1,2,3, G R Strichartz 1,2,3,†
PMCID: PMC434301  PMID: 4530274

Abstract

The effects of monovalent, divalent, and trivalent cations on the binding of tetrodotoxin and saxitoxin to intact nerves and to a preparation of solubilized nerve membranes have been examined. All eight divalent and trivalent cations tested, and the monovalent ions Li+, Tl+, and H+ appear to compete reversibly with the toxins for their binding site. The ability of lithium to reduce toxin binding is paralleled by its ability to reduce tetrodotoxin-sensitive ion fluxes through the nerve membrane. We conclude that the toxins act at a metal cation binding site in the sodium channel and suggest that this site is the principal coordination site for cations (normally Na+ ions) as they pass through the membrane during an action potential. The dissociation constant for Li+ is 0.1-0.2 M and for Na+ > 0.6 M, reflecting the weak binding necessary for rapid passage of sodium ions through the channel.

Keywords: solubilized membrane, receptors, surface charge

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Selected References

These references are in PubMed. This may not be the complete list of references from this article.

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