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  • Title: [Isohistamine and homologs as components of H2-antagonists. 22. H2-antihistaminics].
    Author: Buschauer A, Postius S, Szelenyi I, Schunack W.
    Journal: Arzneimittelforschung; 1985; 35(7):1025-9. PubMed ID: 2864932.
    Abstract:
    Starting with isohistamines and their homologues or from appropriately hydrogenated imidazo[1,2-c]pyrimidines, imidazo[1,2-c] [1,3]diazepines and -diazocines, H2-antihistaminics with cyanoguanidine and 2-nitro-1,1-ethenediamine structure were prepared and tested for their H2-antagonistic activity on the isolated guinea-pig atrium and on the histamine-stimulated acid secretion of the anaesthetized rat. While the cyanoguanidines 3a-c,f were weaker in comparison to cimetidine, or inactive, 12a-e,g-l, 17 and 19 possessed markedly stronger activity, whereby the activity reaches a maximal effect at the rat stomach when cyanoguanidine and imidazole ring are connected with a three-membered chain. The activity of the 2-nitro-1,1-ethenediamines 15b,h,l exceed that of the comparable cyanoguanidines at both test models.
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