Prodrug behaviour of nicotinoylmorphine esters.
Morphine and its nicotinoyl esters, dinicotinoylmorphine (nicomorphine), 6-mononicotinoylmorphine (6-MNM) and 3-mononicotinoylmorphine (3-MNM) were tested in mice for central activity to obtain time-effect profiles of these compounds in rats. Two effects, analgesia with the hot plate test and locomotor stimulation in activity cages were measured and nicomorphine, 6-MNM and 3-MNM were found to have a faster onset of action compared with morphine. The effects of 3-MNM and morphine lasted longer than the effect of nicomorphine and 6-MNM. The prodrug behaviour of 3-MNM and nicomorphine for morphine and 6-MNM, respectively, is discussed.
D000818:Animals; D008297:Male; D051379:Mice; D009022:Morphine Derivatives / Q000493:pharmacokinetics*; D009043:Motor Activity / Q000187:drug effects*; D009539:Nicotinic Acids / Q000493:pharmacokinetics; D004364:Pharmaceutical Preparations; D011355:Prodrugs; D011930:Reaction Time
D009022:Morphine Derivatives; D009539:Nicotinic Acids; D004364:Pharmaceutical Preparations; D011355:Prodrugs; C032054:morphine 6-nicotinate; C053391:morphine 3-nicotinate; C008549:nicomorphine