Orsetti M, Oggero L
Institute of Pharmacology and Pharmacognosy, Pharmacy School, University of Turin, Torino, Italy.
Agents Actions. 1988 Jun;24(1-2):109-13. doi: 10.1007/BF01968087.
The paper reports the pharmacological profile of a new series of ranitidine analogues in which the diaminonitroethene group is replaced by the 2-amino-5(6)-substituted and unsubstituted benzimidazole moieties. These derivatives show a histamine H2-receptor blocking activity comparable to that of the model both in vitro (KB on atria 0.16-1.15 microM) and in vivo (ID50 on the perfused stomach of the anaesthetized rat from 0.34 to 4.10 mumol kg-1 i.v.). The results are consistent with the hypothesis that, at least in the ranitidine analogues, the "urea equivalent" moiety may be replaced by a polar group partially ionized at physiological pH without loss of H2-blocking activity.
该论文报道了一系列新型雷尼替丁类似物的药理学特性，其中二氨基硝基乙烯基团被2-氨基-5（6）-取代和未取代的苯并咪唑部分所取代。这些衍生物在体外（心房KB为0.16 - 1.15微摩尔）和体内（麻醉大鼠灌流胃的ID50为0.34至4.10微摩尔/千克静脉注射）均显示出与模型相当的组胺H2受体阻断活性。结果与以下假设一致：至少在雷尼替丁类似物中，“尿素等效”部分可被在生理pH下部分离子化的极性基团取代，而不会丧失H2阻断活性。
