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Studies on Histaminergic Compounds, IV Non‐isosterism between the Imidazole, Guanidino and Isothiourea Moieties at the H 2 ‐Receptor
Author(s) -
Sterk Geert Jan,
van Der Goot Henk,
Timmerman Henk
Publication year - 1986
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.19863191202
Subject(s) - histaminergic , chemistry , agonistic behaviour , stereochemistry , imidazole , histamine , substituent , receptor , pharmacology , biochemistry , biology , psychology , psychiatry , aggression
S,S'‐Alkylenediisothioureas were found to show only weak agonistic or antagonistic H 2 ‐activity, depending on the length of the alkylene chain. Introduction of a substituent in the amidino parts of both isothiourea groups resulted in a complete loss of the agonistic activity; only inactive compounds or weakly active H 2 ‐antagonists were obtained. Replacing one of the isothiourea groups of the alkylenediisothioureas with n = 2, 3 or 4 by a guanidino group has hardly any or no effect at all on the histamine H 2 ‐activity on the guinea‐pig right atrium. However, extending the alkylene chain of these guanidylalkylisothioureas to n = 5 and 6 results in a strong increase in the H 2 ‐agonistic activity.