Broekkamp C L, Oosterloo S K, Rijk H W
Department of CNS Pharmacology, Organon International B.V., Oss, The Netherlands.
J Pharm Pharmacol. 1988 Jun;40(6):434-7. doi: 10.1111/j.2042-7158.1988.tb06310.x.
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.
对吗啡及其烟酰基酯类化合物，即二烟酰基吗啡（尼可吗啡）、6-单烟酰基吗啡（6-MNM）和3-单烟酰基吗啡（3-MNM），在小鼠身上进行中枢活性测试，以获取这些化合物在大鼠体内的时效曲线。通过热板试验测定镇痛效果，在活动笼中测定运动刺激效果，结果发现与吗啡相比，尼可吗啡、6-MNM和3-MNM起效更快。3-MNM和吗啡的作用持续时间比尼可吗啡和6-MNM更长。分别讨论了3-MNM和尼可吗啡对吗啡和6-MNM的前体药物行为。
