Sato K, Hong Y L, Yang M S, Shibuya T, Kawamoto H, Kitagawa H
Int J Clin Pharmacol Ther Toxicol. 1985 Apr;23(4):204-10.
In order to investigate the central action of zopiclone, the rat brain was divided into 8 regions and the changes in monoamines (MA) in each region were examined. The effect of zopiclone on stress was also examined from changes in brain monoamines under electro-footshock stress load in comparison with that of nitrazepam and flurazepam. The animals were decapitated at 1 h after administration of zopiclone, nitrazepam and flurazepam at each dose of 1 and 10 mg/kg (p.o.). No changes in MA at each region of the brain were noted, but the metabolite, homovanillic acid (HVA) was reduced at the cortex, hippocampus, hypothalamus and cerebellum. 5-hydroxyindoleacetic acid (5-HIAA) was reduced at the amygdala. Noradrenaline (NA) turnover accelerated by electro-footshock stress load was inhibited by zopiclone. From the results of this experiment, it was found that the effects of zopiclone on brain MA were similar to those of nitrazepam and flurazepam: inhibition of 5-HT turnover at the amygdala was common to these three compounds. This result suggests that zopiclone has similar pharmacological properties to benzodiazepines as an antianxiety agent.
为研究佐匹克隆的中枢作用,将大鼠脑部分为8个区域,检测每个区域单胺类物质(MA)的变化。与硝西泮和氟西泮相比,通过电休克应激负荷下脑单胺类物质的变化,研究佐匹克隆对应激的影响。分别以1和10mg/kg(口服)的剂量给予佐匹克隆、硝西泮和氟西泮,给药1小时后断头处死动物。未观察到脑各区域MA有变化,但皮质、海马、下丘脑和小脑的代谢产物高香草酸(HVA)减少。杏仁核中的5-羟吲哚乙酸(5-HIAA)减少。佐匹克隆可抑制电休克应激负荷加速的去甲肾上腺素(NA)周转。从该实验结果发现,佐匹克隆对脑MA的作用与硝西泮和氟西泮相似:这三种化合物对杏仁核5-羟色胺周转的抑制作用是共同的。该结果表明,佐匹克隆作为抗焦虑药具有与苯二氮䓬类相似的药理特性。