Abstract
Batrachotoxinin-A 20-α-benzoate (BTX-B), an analog of the potent depolarizing agent batrachotoxin (BTX), was prepared by selective esterification of naturally occurring batrachotoxinin-A with benzoic acid. BTX-B depolarizes rat phrenic nerve-diaphragm preparations with a time course and concentration dependence virtually indistinguishable from that of BTX. A specific, saturable component of equilibrium binding of [3H]BTX-B to mouse cerebral cortex homogenates was measured, described by an equilibrium dissociation constant of 0.7 µM and a maximum number of binding sites of 90 pmol per gram of tissue (wet weight). Specific binding is inhibited by BTX and other BTX analogs, veratridine, and grayanotoxin but is unaffected by tetrodotoxin and cevine. Under conditions of this assay, neither crude Leiurus quinquestriatus scorpion venom nor purified sea anemone toxin have any effect on specific binding. The data support the conclusion that BTX-B interacts with a recognition site associated with voltage sensitive sodium channels which is identical to the recognition site for BTX.
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This work was supported by a grant from the Alabama Affiliate of the American Heart Association and a NIH grant NS 15617 to G.B.B. and by USPHS grant NS-12063 and Army research office grant 29-78-G-0203 to E.X.A.
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Brown, G.B., Tieszen, S.C., Daly, J.W. et al. Batrachotoxinin-A 20-α-benzoate: A new radioactive ligand for voltage sensitive sodium channels. Cell Mol Neurobiol 1, 19–40 (1981). https://doi.org/10.1007/BF00736037
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DOI: https://doi.org/10.1007/BF00736037