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Evaluation of novel compounds interacting with H2-histamine receptors: Effect on histamine-sensitive adenylate cyclase activity in guinea-pig gastric mucosa

  • Histamine and Kinins
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Abstract

The activity of a number of compounds belonging to the novel class ofN-imidazolylphenyl-N'-alkyl-formamidines on histamine-sensitive adenylate cyclase was evaluated. All substances inhibited histamine-dependent adenylate cyclase activation. The compounds which were investigated in a wider concentration range, i.e. DA 4360, DA 4577, and DA 4626, behaved as simple competitive antagonists, yielding apparentK B values comparable with those estimated in conventional H2-receptor assays. These results provide further evidence for the highly selective H2-receptor antagonism of these new molecules, and confirm the suitability of the histamine-stimulated adenylate cyclase assay in guinea-pig gastric cells as a functionally reduced system for the study of H2 antagonists.

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Authors and Affiliations

  1. Department of Pharmacology, Istituto De Angeli, via Serio 15, 20139, Milan

    Rosella Micheletti & Antonio Giachetti

  2. Institute of Pharmacology and Pharmacognosy, University of Milan, via A. del Sarto 21, 20129, Milan

    Daniela Oliva, Pietro Belfiore & Simonetta Nicosia

Authors
  1. Rosella Micheletti
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  2. Daniela Oliva
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  3. Pietro Belfiore
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  4. Antonio Giachetti
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  5. Simonetta Nicosia
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Micheletti, R., Oliva, D., Belfiore, P. et al. Evaluation of novel compounds interacting with H2-histamine receptors: Effect on histamine-sensitive adenylate cyclase activity in guinea-pig gastric mucosa. Agents and Actions 16, 291–294 (1985). https://doi.org/10.1007/BF01982860

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  • DOI: https://doi.org/10.1007/BF01982860

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