The pharmacology of 20681-S and 20682-S, 6-oxo-N-cyclopropylmethylmorphinans, as narcotic antagonist analgesics.
It has been demonstrated that L-3hydroxy-6-oxo-N-cyclopropylmethylmorphinan methansulfonate (20681-S) and L-3,14-dihydroxy-6-oxo-N-cyclopropylmethylmorphinan methansulfonate (20682-S), have antinociceptive and narcotic antagonistic properties. In the rodent antinociceptive test, the action of 20681-S was more potent and of longer duration than that of morphine and of cyclazocine after subcutaneous or oral administration. The antinociceptive effect of 20682-S ranked between that of morphine and that of pentazocine in the mouse acetic acid-writhing test. Both compounds possessed potent narcotic antagonistic activities, 20682-S being more active than naloxone and oxilorphan and 20681-S being equipotent with cyclazocine. The latent side effects (respiratory depression and fall in blood pressure) and the acute toxicity of 20681-S and 20682-S, were less than those of reference narcotic antagonists or of narcotic antagonist analgesics.
D000700:Analgesics; D000818:Animals; D001522:Behavior, Animal / Q000187:drug effects; D002415:Cats; D005260:Female; D006168:Guinea Pigs; D006439:Hemodynamics / Q000187:drug effects; D007082:Ileum / Q000187:drug effects; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D009019:Morphinans / Q000031:analogs & derivatives / Q000494:pharmacology* / Q000633:toxicity; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D009292:Narcotic Antagonists; D051381:Rats; D012119:Respiration / Q000187:drug effects
C022914:20681-S; C022915:20682-S; D000700:Analgesics; D009019:Morphinans; D009292:Narcotic Antagonists