Trumm K A, Postius S, Szelenyi I, Schunack W
Arzneimittelforschung. 1986 Aug;36(8):1169-74. doi: 10.1002/chin.198650249.
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.
在组胺H2受体拮抗剂的构效关系研究中，制备了N-(3-羟基苯基)胍与5-和7-羟基-四氢异喹啉的拉米替丁类似物衍生物，并在离体豚鼠心房和麻醉大鼠的组胺刺激胃酸分泌实验中测试了它们的H2拮抗活性。研究的另一个目的是考察侧链延长以及用其他H2拮抗成分取代氨基三唑对上述异喹啉衍生物药理数据的影响。所制备的所有化合物在豚鼠心房上仅表现出微弱的H2拮抗活性。在胃酸分泌实验中，尤其是7-羟基-四氢异喹啉异构体表现出显著活性。
