Mühlbachová E, Janků I, Zvárová J, Krebs V, Wenke M
Arzneimittelforschung. 1987 Apr;37(4):394-8.
In vitro lipid-mobilizing activities of morphine (MO) and dynorphin-(1-10) amide (DYA) were compared using adipocytes of young adult rats (body weight 170-200 g, age 50-60 days, diameter of adipocytes 54 +/- 1.12 microns) and of 20-month-old rats (body weight 500-690 g, diameter of adipocytes 99.5 +/- 3.0 microns). The adipokinetic activities of adenosine deaminase (ADA) and dynorphin-(1-13) (DY) were also tested. In the experiments 0.16 units of ADA did not influence basal or stimulated lipolysis, whereas DY exerted a slight but statistically significant adipokinetic effect. In three experimental series the EC50 of MO ranged between 0.89 and 14.60 mumol l-1, the EC50 of DYA in young rats was estimated as 0.8 mumol l-1 and in old animals, 1.3 mumol l-1. Statistically significant differences in the lipid-mobilizing potency between DYA and MO could be observed only in one experimental series in young rats. Expressed in percent of maximum lipolysis induced by isoprenaline, the maximum lipolytic response to DYA in young animals was significantly lower (Emax 26.1 +/- 1.9) when compared to the maximum effect of MO (Emax 76.3 +/- 8.5 and 68.9 +/- 3.5, respectively). Adipocytes of old rats seemed to be more sensitive not only against MO but also against DYA. When studying lipolysis no signs of competitive dualism could be observed in the interaction between MO and DYA. The possibility of two or more independent lipid-mobilizing mechanisms in the effect of the two opioids compared cannot be excluded.
使用年轻成年大鼠(体重170 - 200克,年龄50 - 60天,脂肪细胞直径54±1.12微米)和20月龄大鼠(体重500 - 690克,脂肪细胞直径99.5±3.0微米)的脂肪细胞比较了吗啡(MO)和强啡肽 -(1 - 10)酰胺(DYA)的体外脂质动员活性。还测试了腺苷脱氨酶(ADA)和强啡肽 -(1 - 13)(DY)的脂肪代谢活性。在实验中,0.16单位的ADA不影响基础或刺激的脂解作用,而DY则产生轻微但具有统计学意义的脂肪代谢作用。在三个实验系列中,MO的半数有效浓度(EC50)在0.89至14.60微摩尔/升之间,年轻大鼠中DYA的EC50估计为0.8微摩尔/升,老年动物中为1.3微摩尔/升。仅在年轻大鼠的一个实验系列中观察到DYA和MO之间在脂质动员效力上有统计学显著差异。以异丙肾上腺素诱导的最大脂解作用的百分比表示,与MO的最大作用(分别为Emax 76.3±8.5和68.9±3.5)相比,年轻动物中对DYA的最大脂解反应显著较低(Emax 26.1±1.9)。老年大鼠的脂肪细胞似乎不仅对MO更敏感,而且对DYA也更敏感。在研究脂解作用时,在MO和DYA之间的相互作用中未观察到竞争性二元性的迹象。不能排除所比较的两种阿片类药物作用中存在两种或更多种独立的脂质动员机制的可能性。