Slow wave sleep-inducing effects of first generation H1-antagonists

Koichi Saitou, Yoshio Kaneko, Yukio Sugimoto, Zhong Chen, Chiaki Kamei

Research output: Contribution to journalArticlepeer-review

38 Citations (Scopus)


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.

Original languageEnglish
Pages (from-to)1079-1082
Number of pages4
JournalBiological and Pharmaceutical Bulletin
Issue number10
Publication statusPublished - Oct 1999


  • Brotizolam
  • Chlorpheniramine
  • Diphenhydramine
  • EEG power spectra
  • Promethazine
  • Sleep

ASJC Scopus subject areas

  • Pharmacology
  • Pharmaceutical Science


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