Brain Res. 1990 Jul 23;523(2):325-30.

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

Lin JS, Sakai K, Vanni-Mercier G, Arrang JM, Garbarg M, Schwartz JC, Jouvet M.

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Département de Médecine Expérimentale, INSERM U52, Université Claude Bernard, Lyon, France.

Abstract

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.

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