Characteristics of histamine H1 receptors on HeLa cells.
The affinities of antagonists at histamine H1 receptors on HeLa cells have been determined from inhibition of histamine-induced inositol phosphate formation in intact and from inhibition of [3H]mepyramine binding to HeLa cell membranes. The dissociation constants of mepyramine and (+)-chlorpheniramine were similar to values for binding to H1 receptors in other mammalian tissues, but much lower than the values reported in an earlier study with [3H]mepyramine and HeLa cell membranes. Evidence is presented that under conditions employed in the earlier study the binding of [3H]mepyramine is largely to secondary, non-H1 receptor sites.
Arias-Montaño
J A
JA
Department of Pharmacology, University of Cambridge, UK.
Young
J M
JM
D001665:Binding Sites; D002462:Cell Membrane / Q000378:metabolism*; D002744:Chlorpheniramine / Q000378:metabolism; D006367:HeLa Cells; D006632:Histamine / Q000494:pharmacology; D006801:Humans; D007295:Inositol Phosphates / Q000378:metabolism; D011738:Pyrilamine / Q000378:metabolism; D011969:Receptors, Histamine H1 / Q000378:metabolism*
D007295:Inositol Phosphates; D011969:Receptors, Histamine H1; D002744:Chlorpheniramine; D006632:Histamine; D011738:Pyrilamine