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

JS Lin, K Sakai, G Vanni-Mercier, JM Arrang… - Brain research, 1990 - Elsevier
JS Lin, K Sakai, G Vanni-Mercier, JM Arrang, M Garbarg, JC Schwartz, M Jouvet
Brain research, 1990Elsevier
The effects of histamine H 3-receptor ligands on sleep-waking parameters were studied in
freely moving cats. Oral administration of (R) α-methylhistamine (αMHA), a H 3-agonist,
caused a significant increase in deep slow wave sleep while that of thioperamide, a H 3-
antagonist, enhanced wakefulness in a marked and dose-dependent manner. The arousal
effects of thioperamide were prevented by pretreatment with αMHA or mepyramine, a H 1-
receptor antagonist. The findings support the hypothesis that the histaminergic neurons are …
Abstract
The effects of histamine H3-receptor ligands on sleep-waking parameters were studied in freely moving cats. Oral administration of (R)α-methylhistamine (αMHA), 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 αMHA 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.
Elsevier