title: Specific binding of 3H-tiotidine to histamine H2 receptors in guinea pig cerebral cortex.
abstract: Although the H2 subclass of histamine receptor has been revealed by classical pharmacological approaches, the direct identification of this adenylate cyclase-linked receptor has, despite much effort, remained elusive. Initial studies using 3H-metiamide and 3H-histamine and, subsequently, work from our own laboratory and others using 3H-cimetidine and 3H-ranitidine in various tissues, has shown the unsuitability of these ligands for labelling the H2 receptor. We report here our results using 3H-tiotidine, a more potent H2-antagonist than either cimetidine or ranitidine, and show that this ligand meets the criteria for labeling the H2 receptor in guinea pig cerebral cortex membranes.
mesh_terms: D000818:Animals; D001667:Binding, Competitive; D002540:Cerebral Cortex / Q000378:metabolism*; D002927:Cimetidine / Q000031:analogs & derivatives*; D006146:Guanidines / Q000378:metabolism*; D006168:Guinea Pigs; D006635:Histamine H2 Antagonists / Q000378:metabolism*; D007700:Kinetics; D011968:Receptors, Histamine / Q000378:metabolism*; D011970:Receptors, Histamine H2 / Q000378:metabolism*; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000378:metabolism*
chemical_list: D006146:Guanidines; D006635:Histamine H2 Antagonists; D011968:Receptors, Histamine; D011970:Receptors, Histamine H2; D013844:Thiazoles; D002927:Cimetidine; C023990:tiotidine