Labeling of histamine H1-receptors in the brain of the living mouse.
Labeling of cerebral H1-receptors is obtained following i.v. administration of [3H]mepyramine in tracer dose as shown by saturability, stereospecificity, regional distribution and pharmacological specificity. Cerebral H1-receptors are occupied following administration of most H1-antihistamines at low therapeutic dosage, which probably accounts for the sedative side-effects of these agents.
D000631:Aminopyridines / Q000378:metabolism*; D000818:Animals; D001665:Binding Sites; D001667:Binding, Competitive; D001921:Brain / Q000378:metabolism*; D006634:Histamine H1 Antagonists / Q000378:metabolism; D008297:Male; D051379:Mice; D011738:Pyrilamine / Q000378:metabolism*; D011968:Receptors, Histamine / Q000378:metabolism*; D011969:Receptors, Histamine H1 / Q000378:metabolism*
D000631:Aminopyridines; D006634:Histamine H1 Antagonists; D011968:Receptors, Histamine; D011969:Receptors, Histamine H1; D011738:Pyrilamine