Involvement of histaminergic neurons in arousal mechanisms demonstrated with H3-receptor ligands in the cat

Brain Res. 1990 Jul 23;523(2):325-30. doi: 10.1016/0006-8993(90)91508-e.


The effects of histamine H3-receptor ligands on sleep-waking parameters were studied in freely moving cats. Oral administration of (R)alpha-methylhistamine (alpha MHA), a H3-agonist, caused a significant increase in deep slow wave sleep while that of thioperamide, a H3-antagonist, enhanced wakefulness in a marked and dose-dependent manner. The arousal effects of thioperamide were prevented by pretreatment with alpha MHA or mepyramine, a H1-receptor antagonist. The findings support the hypothesis that the histaminergic neurons are critically involved in arousal mechanisms and suggest that H3-receptors play an active part in these mechanisms by regulating histamine transmission.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Arousal* / drug effects
  • Brain / drug effects
  • Brain / physiology*
  • Cats
  • Electroencephalography
  • Female
  • Ligands
  • Male
  • Methylhistamines / pharmacology*
  • Neurons / physiology*
  • Piperidines / pharmacology
  • Receptors, Histamine / drug effects
  • Receptors, Histamine / metabolism
  • Receptors, Histamine / physiology*
  • Receptors, Histamine H3
  • Reference Values
  • Sleep / drug effects


  • Ligands
  • Methylhistamines
  • Piperidines
  • Receptors, Histamine
  • Receptors, Histamine H3
  • thioperamide
  • N-methylhistamine