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Neosurugatoxin, a Specific Antagonist of Nicotinic Acetylcholine Receptors
Author(s) -
Hayashi E.,
Isogai M.,
Kagawa Y.,
Takayanagi N.,
Yamada S.
Publication year - 1984
Publication title -
journal of neurochemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.75
H-Index - 229
eISSN - 1471-4159
pISSN - 0022-3042
DOI - 10.1111/j.1471-4159.1984.tb02817.x
Subject(s) - nicotinic agonist , oxotremorine , muscarinic acetylcholine receptor , nicotine , acetylcholine receptor , chemistry , acetylcholine , receptor , nicotinic antagonist , forebrain , agonist , cholinergic , neurotoxin , binding site , antagonist , pharmacology , endocrinology , medicine , biology , biochemistry , central nervous system
Neosurugatoxin (NSTX) (3 n M ‐30 n M ), recently isolated from the Japanese ivory mollusc ( Babylonia japonica ) exerted a potent antinicotinic action in the isolated guinea pig ileum. Specific [ 3 H]nicotine binding to rat forebrain membranes was saturable, reversible, and of high affinity. Nicotinic cholinergic agonists exhibited a markedly greater affinity for [ 3 H]nicotine binding sites than a muscarinic agonist, oxotremorine. Although α‐bungarotoxin had no effect on [ 3 H]nicotine binding, low concentrations (1 n M ‐1 μ M ) of NSTX inhibited [ 3 H]nicotine binding in the forebrain membranes and its IC 50 value was 69 ± 6 n M . On the other hand, NSTX did not affect muscarinic receptor binding in the brain. These data indicate that NSTX may be of appreciable interest as a neurotoxin with a selective affinity for ganglionic nicotinic receptors.