Antitussive activity and other related pharmacological properties of d-3-methyl-N-methylmorphinan (AT-17).
Antitussive activity and some other related pharmacological properties of d-3-methyl-N-methylmorphinan were studied. Toxic symptoms in mice and dogs were due to the CNS excitation. Acute toxicity of (AT-17) in mice was slightly (s.c.) or far (p.o.) weaker than that of codeine, but it was three times as toxic as codeine in dogs (i.v.). Antitussive efficacy was about 40% of that of codeine in dogs, whereas 77% as potent as codeine in cats. It showed no relaxing effect on the bronchial muscle of guinea pigs in either normal tone or histamine-induced spasms. It had analgesic effect 1/3 as potent as codeine in mice but it was not antagonized by levallorphan. The prolongation of hexobarbital sleeping time by AT-17 was similar extent to that by codeine. Anti-electroshock effect was half as potent as that of phenobarbital. The inhibitory effect on the transportation of intestinal contents in mice was far weaker than that of codeine. Effect on the respiratory and circulatory systems were also investigated.
D000698:Analgesia; D000818:Animals; D000996:Antitussive Agents; D001794:Blood Pressure / Q000187:drug effects; D001980:Bronchi / Q000187:drug effects / Q000378:metabolism; D002415:Cats; D003061:Codeine / Q000494:pharmacology; D003915:Dextromethorphan / Q000494:pharmacology; D004285:Dogs; D005260:Female; D006168:Guinea Pigs; D066298:In Vitro Techniques; D007422:Intestines / Q000187:drug effects; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D009019:Morphinans / Q000494:pharmacology* / Q000633:toxicity; D009119:Muscle Contraction / Q000187:drug effects; D009129:Muscle Tonus / Q000187:drug effects; D011817:Rabbits; D012119:Respiration / Q000187:drug effects; D012640:Seizures / Q000188:drug therapy; D012890:Sleep / Q000187:drug effects; D014132:Trachea / Q000187:drug effects; D014666:Vasomotor System / Q000187:drug effects
D000996:Antitussive Agents; D009019:Morphinans; D003915:Dextromethorphan; D003061:Codeine