Antonelli T, Beani L, Bianchi C, Rando S, Simonato M, Tanganelli S
Br J Pharmacol. 1986 Dec;89(4):853-60. doi: 10.1111/j.1476-5381.1986.tb11191.x.
The effects of naloxone on acetylcholine (ACh) and gamma-aminobutyric acid (GABA) outflow from the cerebral cortex of freely moving, morphine-dependent guinea-pigs was studied. The cortical efflux of ACh in chronically-treated guinea-pigs was about half of that of normal animals. GABA efflux was unaffected. During opioid withdrawal precipitated by naloxone (0.1-10 mg kg-1, i.p.) the guinea-pigs showed jumping, hyperactivity and wet dog shakes, the intensity of which was directly related to the dose of naloxone. The withdrawal syndrome was accompanied by a dose-dependent increase in ACh release and reduction in GABA outflow; ACh release was increased by naloxone at doses lower (0.1-3 mg kg-1) than those acting on GABA efflux (1-10 mg kg-1). Atropine (10 mg kg-1) and diazepam (5 mg kg-1) did not prevent GABA and ACh changes.
研究了纳洛酮对自由活动的吗啡依赖豚鼠大脑皮质乙酰胆碱（ACh）和γ-氨基丁酸（GABA）释放的影响。长期接受治疗的豚鼠皮质ACh流出量约为正常动物的一半。GABA流出量未受影响。在用纳洛酮（0.1 - 10 mg kg-1，腹腔注射）诱发阿片类物质戒断期间，豚鼠表现出跳跃、多动和湿狗样抖动，其强度与纳洛酮剂量直接相关。戒断综合征伴有ACh释放剂量依赖性增加和GABA流出量减少；纳洛酮在低于作用于GABA流出量的剂量（0.1 - 3 mg kg-1）时即可增加ACh释放，而作用于GABA流出量的剂量为（1 - 10 mg kg-1）。阿托品（10 mg kg-1）和地西泮（5 mg kg-1）不能阻止GABA和ACh的变化。
