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

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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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Authors and Affiliations

  1. Hoechst Pharmaceutical Research Laboratories, Hoechst UK Ltd, Walton Manor, Walton, Milton Keynes, Bucks, MK7 7AJ, UK

    Gillian A. Gajtkowski, D. B. Norris, T. J. Rising & T. P. Wood

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  1. Gillian A. Gajtkowski
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  2. D. B. Norris
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  3. T. J. Rising
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  4. T. P. Wood
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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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