Activities of morphinone and N-(cyclopropylmethyl)normorphinone at opioid receptors.
Morphinone (3) and N-(cyclopropylmethyl)normorphinone (4) were synthesized and tested on electrically stimulated smooth muscle preparations (guinea pig ileum and mouse vas deferens) and in mice. Compound 3 behaved as an agonist and 4 as an antagonist in vitro and in vivo. No pronounced nonequilibrium agonist or antagonist activity was observed with either compound.
D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D006168:Guinea Pigs; D004091:Hydromorphone / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D007082:Ileum / Q000187:drug effects; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D051379:Mice; D011957:Receptors, Opioid / Q000187:drug effects / Q000502:physiology*; D013329:Structure-Activity Relationship; D014649:Vas Deferens / Q000187:drug effects
D007202:Indicators and Reagents; D011957:Receptors, Opioid; C036083:morphinone; C042928:N-(cyclopropylmethyl)normorphinone; D004091:Hydromorphone