PMID: 6103536Mar 1, 1980Paper

Binding of sea anemone toxin to receptor sites associated with gating system of sodium channel in synaptic nerve endings in vitro

Proceedings of the National Academy of Sciences of the United States of America
J P VincentM Lazdunski

Abstract

Iodination of toxin II from the sea anemone Anemonia sulcata gives a labeled monoiododerivative that retains 80% of the original neurotoxicity. This derivative binds specifically to rat brain synaptosomes at 20 degrees C and pH 7.4 with a second-order rate constant of association ka = 4.6 x 10(4) M-1 sec-1 and a first-order rate constant of dissociation kd = 1.1 x 10(-2) sec-1. The binding occurs on the Na+ channel at a binding site distinct from that of other gating system toxins like batrachotoxin, veratridine, grayanotoxin, aconitine, and pyrethroids. The maximal binding capacity Bmax is 3.2 pmol/mg of protein (i.e., about two sea anemone toxin binding sites per tetrodotoxin binding site) and the Kd is 240 nM for the monoiododerivative and 150 nM for the native toxin. Corresponding binding parameters for the association of a 125I-labeled derivative of toxin II from the scorpion Androctonus australis Hector are Bmax = 0.3 pmol/mg of protein and Kd = 1 nM, whereas the Kd of the unmodified scorpion toxin is 0.6 nM. Competition experiments involving scorpion toxins, sea anemone toxins, and synaptosomes demonstrate that, although the sea anemone toxin is able to displace the scorpion toxin bound to synaptosomes, the scorpion toxi...Continue Reading

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Citations

Jun 1, 1993·Pflügers Archiv : European journal of physiology·J A WasserstromK N Liberty
Jan 1, 1988·Pflügers Archiv : European journal of physiology·A WarashinaT Ogura
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