Macrocyclic Polyamines as a Possible Chemical Model for Histamine H_2-Receptors

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An 18-membered macrocyclic hexaamine, [18] aneN_6,interacts with histamine and its H_2-agonist dimaprit at physiological pH to yield stable 1 : 1 complexes with simultaneous liberation of H^+, which mimics the histamine H_2-receptor-agonist interaction and the resulting gastric acid secretion. The polyamine H_2-receptor model does not interact with the histamine H_1-agonist 2-pyridylethylamine. Our model does interact with the H_2-antagonists cimetidine, metiamide, famotidine and ranitidine to form more stable 1 : 1 complexes than with the H_2-agonists, which offers a possible chemical model for the pharmacological ability of the H_2-antagonists to competitively block H_2-receptors and inhibit the gastric acid secretion induced by histamine. The known structural features distinguishing between histamie H_1-and H_2-agonist, and between histamine H_2-agonist and -antagonist are reevaluated in terms of our model.
社団法人日本薬学会の論文
1984-09-25