Affinities of histamine H1-antagonists in guinea pig brain: similarity of values determined from [3H]mepyramine binding and from inhibition of a functional response.
Affinity constants for five antagonists at histamine H1-receptors in guinea pig brain have been determined from inhibition of the potentiation by histamine of the adenosine-induced accumulation of cyclic AMP in cerebral cortical slices. This action of histamine appeared to be mediated solely through H1-receptors. The affinity constants obtained were similar to those determined on peripheral H1-receptors and from inhibition of high-affinity [3H]mepyramine binding. This provides strong evidence that at least some of the [3H]mepyramine binding sites in guinea pig brain can be identified with functional H1-receptors.
D000631:Aminopyridines / Q000378:metabolism*; D000818:Animals; D001667:Binding, Competitive; D001921:Brain / Q000378:metabolism*; D005260:Female; D006168:Guinea Pigs; D006634:Histamine H1 Antagonists / Q000494:pharmacology*; D007700:Kinetics; D008297:Male; D011738:Pyrilamine / Q000378:metabolism*; D011968:Receptors, Histamine / Q000378:metabolism*; D011969:Receptors, Histamine H1 / Q000378:metabolism*; D013329:Structure-Activity Relationship
D000631:Aminopyridines; D006634:Histamine H1 Antagonists; D011968:Receptors, Histamine; D011969:Receptors, Histamine H1; D011738:Pyrilamine