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研究化合物H1208对小鼠的镇静催眠作用,并对其机制进行初步探索。通过测定H1208对小鼠自主活动、睡眠潜伏期及睡眠持续时间的影响,评价其中枢镇静及催眠作用;通过监测小鼠脑电及肌电,分析H1208对睡眠成分的影响;并应用高效液相色谱-电化学检测法测定小鼠大脑皮层、纹状体及下丘脑内单胺类神经递质含量的变化。结果表明,与溶剂对照组比较,腹腔注射H1208(5和25 mg·kg-1,ip)能显著抑制小鼠的自主活动,抑制率分别为56.7%和80.2%。H1208(30和60 mg·kg-1,ip)可诱导小鼠睡眠,增加非快动眼睡眠,缩短快动眼睡眠时间,显著降低小鼠纹状体和大脑皮层内多巴胺及大脑皮层内5-羟色胺含量。结果提示,H1208具有强效的镇静催眠作用;降低脑内神经递质多巴胺、5-羟色胺水平可能是其发挥镇静催眠作用的机制之一。
To study the sedative and hypnotic effects of compound H1208 on mice, and to explore its mechanism. The effects of H1208 on the spontaneous activity, sleep latency and duration of sleep were evaluated to evaluate the central sedative and hypnotic effects of H1208. The effects of H1208 on sleep composition were analyzed by monitoring the electroencephalogram and electromyography. The effects of H1208 on sleep composition were analyzed by HPLC. Determination of monoamine neurotransmitters in cerebral cortex, striatum and hypothalamus of mice by electrochemical detection. The results showed that intraperitoneal injection of H1208 (5 and 25 mg · kg-1, ip) could significantly inhibit the autonomic activity of mice compared with the solvent control group, with the inhibition rates of 56.7% and 80.2%, respectively. H1208 (30 and 60 mg · kg-1, ip) can induce sleep in mice, increase non-REM sleep, shorten the time of REM sleep, significantly reduce dopamine and cerebral cortex in mouse striatum and cerebral cortex.5 Serotonin content. The results suggest that H1208 has potent sedative and hypnotic effects. Decreasing dopamine and serotonin, which are neurotransmitters in the brain, may be one of the mechanisms by which sedative and hypnotic effects are exerted.