[Tetrahydroisoquinolines as components of H2-antagonists. 27. H2-antihistaminics].
In studies on structure-activity relationships of histamine H2-receptor antagonists, lamtidine-analogue derivatives of N-(3-hydroxyphenyl)guanidine and 5- and 7-hydroxy-tetrahydroisoquinoline 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. A further aim of the investigations was to examine the influence of a lengthening of the side-chain as well as the substitution of the aminotriazole with other H2-antagonistic components, on the pharmacological data of the above-mentioned isoquinoline derivatives. All compounds made showed only little H2-antagonistic activity on the guinea-pig atrium. At the acid secretion a noticeable activity especially of the 7-hydroxy-tetrahydroisoquinoline isomers could be observed.
D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D005744:Gastric Acid / Q000378:metabolism; D006168:Guinea Pigs; D006321:Heart / Q000187:drug effects; D006635:Histamine H2 Antagonists / Q000138:chemical synthesis*; D007082:Ileum / Q000187:drug effects; D066298:In Vitro Techniques; D007546:Isoquinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D008297:Male; D009130:Muscle, Smooth / Q000187:drug effects; D051381:Rats; D011919:Rats, Inbred Strains
D006635:Histamine H2 Antagonists; D007546:Isoquinolines
Tetrahydroisochinoline als Bausteine von H2-Antagonisten. 27. Mitteilung: H2-Antihistaminika.