STRUCTURE AND ACTIVITY IN TETRODOTOXIN DERIVATIVES

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Abstract
Pharmacological properties of 9 compounds related to tetrodotoxin were investigated. The compounds were tetrodotoxin, desoxytetrodotoxin, methoxy-tetrodotoxin, ethoxytetrodotoxin, tetrodaminotoxin, anhydrotetrodotoxin, 11 -monoformylanhydrotetrodotoxin, 6,11 -diacetylanhydrotetrodotoxin, and tetrodonic acid. They all showed similar pharmacological properties in symptomatology in mice, blood pressure and respiration experiments in cats and in vitro tests on nerve conduction blocking activity in the frog sciatic nerve and on spasmolytic activity in guinea pig ileum. On the basis of existing great quantitative differences in the pharmacological activity, the structure-activity relation in tetrodotoxin was discussed.