Histamine H1-receptors labeled in vivo: antidepressant and antihistamine interactions.

3H-Mepyramine labels specific histamine H1-receptors in brains of mice after intravenous injection. The potencies of H1-antihistamines in reducing 3H-mepyramine binding in vivo correspond to their pharmacological activities and show parallels with their affinities for 3H-mepyramine binding sites in isolated brain membranes. Several antidepressants are potent in competing for 3H-mepyramine binding in vivo as well as in vitro.