Horita A, Carino M A, Chinn C
Department of Pharmacology, University of Washington School of Medicine, Seattle 98195.
Neuropharmacology. 1989 May;28(5):481-6. doi: 10.1016/0028-3908(89)90083-x.
Fentanyl (20 micrograms/kg i.p.), administered to naltrexone-pretreated, pentobarbital-anesthetized rats, produced a shortening of the duration of narcosis. This analeptic effect was blocked by atropine, but not by methylatropine, indicating that a central cholinergic mechanism was involved. Fentanyl also increased sodium-dependent high affinity uptake of choline activity in the hippocampus and cortex that had been depressed by the barbiturate. Injection of 0.8 ng of fentanyl into the pontis oralis in the pontine reticular formation also produced analepsis in naltrexone-pretreated, pentobarbitalized rats. Hippocampal EEG recordings also showed the appearance of cholinergically-mediated theta activity, which was indicative of arousal activity in the hippocampus. These results suggest that fentanyl, in addition to possessing potent opiate activity, also activates a nonopioid-mediated central cholinergic arousal system.
给经纳曲酮预处理、戊巴比妥麻醉的大鼠腹腔注射芬太尼（20微克/千克），可缩短麻醉持续时间。这种苏醒作用被阿托品阻断，但未被甲基阿托品阻断，表明涉及中枢胆碱能机制。芬太尼还增加了海马体和皮质中被巴比妥酸盐抑制的钠依赖性高亲和力胆碱摄取活性。向脑桥网状结构的脑桥口腔部注射0.8纳克芬太尼，也能使经纳曲酮预处理、戊巴比妥麻醉的大鼠产生苏醒作用。海马体脑电图记录还显示出现了胆碱能介导的θ活动，这表明海马体中有觉醒活动。这些结果表明，芬太尼除了具有强效阿片类活性外，还激活了非阿片类介导的中枢胆碱能觉醒系统。
