Pharmacological studies on a new 1-benzoyloxy-alkylaminocycloalkane derivative (YAU-17) with special reference to its mucosa anesthetic activity.
A new compound, dl-cis-1-benzoyloxy-2-dimethylamino-1,2,3,4-tetrahydronaphthalane (YAU-17) was found to produce sciatic nerve block, corneal and intradermal anesthesia in guinea-pigs, which markedly exceeded the effect of procaine and lidocaine. YAU-17, when given orally to mice, was much less toxic than any other drugs tested, though YAU-17 showed a considerably high acute toxicity by i.v. route. Oral administration of YAU-17 was effective in antagonizing the emetic response of dogs to intragastric phenylalanine isopropyl ester, but produced no distinct inhibition against vomiting elicited by oral copper sulfate. Furthermore, it possessed a spasmolytic activity which was comparable to that of papaverine, and showed an effect of suppressing the mucosal intrinsic reflex in the dog intestine. These pharmacological properties of YAU-17 were qualitatively similar to those of oxetacaine which was used as one of the reference compounds.