Slow wave sleep-inducing effects of first generation H1-antagonists.
Slow wave sleep-inducing effects of first generation H1-antagonists.
复制标题
第一代 H1 拮抗剂的慢波睡眠诱导作用。
DOI：
10.1248/bpb.22.1079
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发表时间：
1999
影响因子：
2
通讯作者：
C. Kamei
中科院分区：
文献类型：
--
作者：
K. Saitou;Y. Kaneko;Y. Sugimoto;Z. Chen;C. Kamei
本研究旨在了解第一代组胺H1拮抗剂是否为有效的镇静催眠药物。以大鼠额叶皮质Delta频段(0~4 Hz)和海马区theta频段(4~8 Hz)脑电功率谱增加作为睡眠指标。这项研究中使用的H1拮抗剂导致睡眠潜伏期的缩短和睡眠持续时间的延长(慢波睡眠)。H1受体拮抗剂和溴唑仑可降低慢波睡眠中的快速眼动睡眠频率。H1受体拮抗剂缩短睡眠潜伏期的作用由大到小依次为promethazine>；chlorpheniramine>；diphenhydramine和吡拉明，延长睡眠时间的作用依次为chlorpheniramine>；promethazine>；diphenhydramine和吡拉明。与H1受体拮抗剂相比，溴唑仑的作用更强，对睡眠潜伏期和持续时间的影响分别为14-18倍和4-14倍。这些结果清楚地表明，H1-拮抗剂作为镇静催眠药物对轻、中度失眠有效。
The present study was performed to see if first-generation histamine H1-antagonists are useful sedative-hypnotic drugs. Increases in electroencephalogram (EEG) power spectra of the delta band (0-4 Hz) at the frontal cortex and theta band (4-8 Hz) at the hippocampus in rats were used as an indexes of sleep. The H1-antagonists used in this study resulted in a decrease in sleep latency and an increase in sleep duration (slow wave sleep). The rate of REM (rapid eye movement) sleep during slow wave sleep was decreased by H1-antagonists and brotizolam. The order of potency of H1-antagonists for the reduction in sleep latency (from greatest to least) was promethazine>chlorpheniramine>diphenhydramine and pyrilamine, and that for the increase in sleep duration was chlorpheniramine>promethazine>diphenhydramine and pyrilamine. Brotizolam was more potent than these H1-antagonists, with 14-18-fold and 4-14-fold greater effects on sleep latency and duration, respectively. These results clearly show that H1-antagonists are effective in mild to moderate insomnia as sedative-hypnotic drugs.