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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 approaches1,2, the direct identification of this adenylate cyclase-linked receptor has, despite much effort, remained elusive. Initial studies using 3H-metiamide and 3H-histamine3,4 and, subsequently, work from our own laboratory and others using 3H-cimetidine5–8 and 3H-ranitidine9 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 ranitidine10, and show that this ligand meets the criteria for labelling the H2 receptor in guinea pig cerebral cortex membranes.

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Gajtkowski, G., Norris, D., Rising, T. et al. Specific binding of 3H-tiotidine to histamine H2 receptors in guinea pig cerebral cortex. Nature 304, 65–67 (1983). https://doi.org/10.1038/304065a0

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