Specific binding of 3H-tiotidine to histamine H2 receptors in guinea pig cerebral cortex.

摘要: Although the H2 subclass of histamine receptor has been revealed by classical pharmacological approaches1,2, direct identification this adenylate cyclase-linked has, despite much effort, remained elusive. Initial studies using 3H-metiamide and 3H-histamine3,4 and, subsequently, work from our own laboratory others 3H-cimetidine5–8 3H-ranitidine9 in various tissues, shown unsuitability these ligands for labelling receptor. We report here results 3H-tiotidine, a more potent H2-antagonist than either cimetidine or ranitidine10, show that ligand meets criteria guinea pig cerebral cortex membranes.