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

FEBS Letters

Lazdunski, Michel¹  Lombet, Alain¹  Bidard, Jean-Noël¹ 

[1] Centre de Biochimie du CNRS, Parc Valrose,06034 Nice Cedex, France

关键词: Ciguatoxin;    Na channel;    Ciguatera;    Brevetoxin;    Receptor;    Pyrethroid;    AS2;    Anemonia sulcata toxin 2;    [3H]BTX-B;    [3H]batrachotoxinin A 20-α-benzoate;    CgTx;    ciguatoxin;    PbTx;    brevetoxin (Ptychodiscus brevis toxin);    TTX;    tetrodotoxin;   

DOI  :  10.1016/0014-5793(87)80252-1

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

Binding studies indicate that ciguatoxin and brevetoxin allosterically enhance in a very similar way the binding of [³H]batrachotoxinin A 20-α-benzoate to the neuronal Na⁺ channel protein. Moreovr 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.

【 授权许可】

Unknown