title: The use of an in vitro binding assay to predict histamine H2-antagonist activity.
abstract: Thirty-seven compounds were evaluated for their ability to inhibit histamine stimulated adenylate cyclase and to inhibit 3H-tiotidine binding. The compounds examined included a number of known H2-antagonists and a number of potential H2-antagonists of diverse chemical structure. The correlation between the Ki values from the binding assay and from the inhibition of adenylate cyclase was calculated to be r = 0.99, p less than 0.001. Thus 3H-tiotidine binding in guinea-pig cerebral cortex can be used to give a valid assessment of histamine H2-receptor activity.
authors.forename: D B
authors.initials: DB
authors.lastname: Norris
authors.forename: G A
authors.initials: GA
authors.lastname: Gajtkowski
authors.forename: T P
authors.initials: TP
authors.lastname: Wood
authors.forename: T J
authors.initials: TJ
authors.lastname: Rising
mesh_terms: D000067956:Adenylyl Cyclase Inhibitors; D000818:Animals; D002927:Cimetidine / Q000031:analogs & derivatives / Q000378:metabolism; D005260:Female; D006168:Guinea Pigs; D006635:Histamine H2 Antagonists / Q000494:pharmacology*; D066298:In Vitro Techniques; D008297:Male; D011970:Receptors, Histamine H2 / Q000378:metabolism; D014316:Tritium
chemical_list: D000067956:Adenylyl Cyclase Inhibitors; D006635:Histamine H2 Antagonists; D011970:Receptors, Histamine H2; D014316:Tritium; D002927:Cimetidine; C023990:tiotidine