[Isohistamine and homologs as components of H2-antagonists. 22. H2-antihistaminics].
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.
Buschauer
A
A
Postius
S
S
Szelenyi
I
I
Schunack
W
W
D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D005753:Gastric Mucosa / Q000378:metabolism; D006168:Guinea Pigs; D006632:Histamine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D006635:Histamine H2 Antagonists / Q000138:chemical synthesis*; D066298:In Vitro Techniques; D008297:Male; D009131:Muscle, Smooth, Vascular / Q000187:drug effects; D009200:Myocardial Contraction / Q000187:drug effects; D051381:Rats; D011919:Rats, Inbred Strains
D006635:Histamine H2 Antagonists; C040604:isohistamine; D006632:Histamine
Isohistamine und Homologe als Bausteine von H2-Antagonisten. 22. Mitt.: H2-Antihistaminika.