Histamine-induced constriction and dilatation of rabbit middle cerebral arteries in vitro: role of the endothelium.

We studied the effects of histamine on perfused rabbit middle cerebral arteries in vitro. Intact and endothelium-denuded preparations were compared. Histamine caused concentration-dependent constrictions in intact vessels which were competitively inhibited by an H1 receptor antagonist. This constriction was potentiated by either H2-receptor blockade or endothelium denudation. The greatest potentiation was observed with intraluminal as opposed to extraluminal administration. The H1 receptor agonist pyridylethylamine induced similar concentration-dependent constriction in intact and denuded preparations. After preconstriction, histamine, in the presence of an H1 receptor antagonist, dilated intact vessels to a maximum of 45.1%, and endothelium-denuded vessels to a maximum of 22% (p less than 0.02). We conclude that rabbit middle cerebral arteries possess H1 constrictory and H2 dilatory receptors, and that many of the H2 dilatory receptors are situated on the endothelial cells.