Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
Macrocyclic Polyamines as a Possible Chemical Model for Histamine H2-Receptors
EIICHI KIMURATOHRU KOIKEMUTSUO KODAMA
Author information
Keywords: receptor model.
JOURNAL FREE ACCESS

1984 Volume 32 Issue 9 Pages 3569-3578

Details
Abstract
An 18-membered macrocyclic hexaamine, [18] aneN6, interacts with histamine and its H2-agonist dimaprit at physiological pH to yield stable 1 : 1 complexes with simultaneous liberation of H+, which mimics the histamine H2-receptor-agonist interaction and the resulting gastric acid secretion. The polyamine H2-receptor model does not interact with the histamine H1-agonist 2-pyridylethylamine. Our model does interact with the H2-antagonists cimetidine, metiamide, famotidine and ranitidine to form more stable 1 : 1 complexes than with the H2-agonists, which offers a possible chemical model for the pharmacological ability of the H2-antagonists to competitively block H2-receptors and inhibit the gastric acid secretion induced by histamine. The known structural features distinguishing between histamie H1-and H2-agonist, and between histamine H2-agonist and -antagonist are reevaluated in terms of our model.
Content from these authors
© The Pharmaceutical Society of Japan
Previous article Next article
feedback
Top