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Structure-Activity Relationship of Lyoniol-A and Related Compounds in Association with the Excitatory Effect on Muscle Spindle Afferents

1974; Pharmaceutical Society of Japan; Volume: 22; Issue: 4 Linguagem: Inglês

10.1248/cpb.22.884

1347-5223

Hideomi Fukuda, Yoshihisa Kudo, Hideki Ono, Masaiti Yasue, Jinsaku Sakakibara, Takeshi Kato,

Marine Sponges and Natural Products

The action on muscle spindle afferents, sialogogous action and acute toxicity of lyoniol-A and eleven related compounds were determined. The excitatory action on muscle spindle afferents were measured as the increase in frequencies of the afferent discharge from de-efferented muscle spindles in anesthetized rats. LD50-and salivationtests were conducted using mice. Of the compounds studied, lyoniol-A, lyoniol-B, dihydrolyoniol-B, grayanotoxin-I and grayanotoxin-III were more potent than suxamethonium, an established muscle spindle excitant, in causing an increase in afferent discharges from muscle spindles. The action on muscle spindle afferents and acute toxicity of the compounds studied were roughly parallel. The relationship between structure and activity was discussed.