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.
D015081:2-Naphthylamine / Q000031:analogs & derivatives / Q000494:pharmacology / Q000633:toxicity; D000779:Anesthetics, Local / Q000633:toxicity; D000818:Animals; D000932:Antiemetics; D001565:Benzoates / Q000494:pharmacology* / Q000633:toxicity; D003315:Cornea / Q000187:drug effects; D004285:Dogs; D005769:Gastrointestinal Motility / Q000187:drug effects; D006168:Guinea Pigs; D007413:Intestinal Mucosa / Q000187:drug effects*; D007928:Lethal Dose 50; D051379:Mice; D009407:Nerve Block; D010276:Parasympatholytics; D012584:Sciatic Nerve / Q000187:drug effects
D000779:Anesthetics, Local; D000932:Antiemetics; D001565:Benzoates; D010276:Parasympatholytics; D015081:2-Naphthylamine