Yamaura T, Shibata M, Inaba N, Onodera S, Chida Y, Ohnishi H
Pharmaceuticals Research Laboratories, Fujirebio, Inc., Tokyo, Japan.
Nihon Yakurigaku Zasshi. 1992 Jun;99(6):401-10. doi: 10.1254/fpj.99.401.
We examined the anti-ulcer effects of FRG-8813, a new type histamine H2-receptor antagonist, on various experimental gastric and duodenal lesions in rats. FRG-8813, administered orally, inhibited the formation of lesions dose-dependently in experimental models with the exception of the Shay ulcer model. The anti-ulcer potency of FRG-8813 was 4 approximately 10 times greater than that of cimetidine when the ED50 values of both compounds were compared. Famotidine and cimetidine inhibited lesion formation at higher doses than the anti-secretory doses. The anti-ulcer action of FRG-8813, however, appeared at even lower doses than those of anti-secretory action. These results suggest that FRG-8813 is able to prevent lesion formation with anti-secretory action plus other mechanisms unlike typical histamine H2-receptor antagonists.
我们研究了新型组胺H2受体拮抗剂FRG - 8813对大鼠各种实验性胃和十二指肠损伤的抗溃疡作用。口服给予FRG - 8813，在除沙伊氏溃疡模型外的实验模型中，其对损伤形成的抑制作用呈剂量依赖性。当比较两种化合物的半数有效剂量（ED50）值时，FRG - 8813的抗溃疡效力比西咪替丁大约高4至10倍。法莫替丁和西咪替丁在高于抗分泌剂量时抑制损伤形成。然而，FRG - 8813的抗溃疡作用在甚至低于抗分泌作用的剂量时就出现了。这些结果表明，与典型的组胺H2受体拮抗剂不同，FRG - 8813能够通过抗分泌作用以及其他机制来预防损伤形成。
