Takano K, Sugiyama S, Goto H, Nakazawa S, Ozawa T
Department of Internal Medicine, Faculty of Medicine, University of Nagoya, Japan.
Arzneimittelforschung. 1988 Mar;38(3):364-6.
A quantitative and rapid method was developed for determination of tissue prostaglandin (PG) levels using reverse phase high performance liquid chromatography. Using this method, we investigated the effects of famotidine (YM-11170), an H2-blocker, on changes in gastric mucosal PG levels induced by water immersion stress in rats. Gastric mucosal phospholipase (PLase) activity was also estimated. Four kinds of PGs, i.e., 6-keto-PGF1a, PGE2, PGF2a, and PGD2 were detected in gastric mucosa. 6 h water immersion stress induced decreases in all of them at a similar degree, the reduction being about 70% of the control value. Decreases in PLase activity were also observed in rats with 6 h stress. Pretreatment with famotidine prevented decreases in levels of PGs, which are known to have cytoprotective effect, and also maintained PLase activity. These results indicate that famotidine exerts its anti-ulcer action via maintenance of PG levels and PLase activity.
开发了一种使用反相高效液相色谱法测定组织前列腺素(PG)水平的定量快速方法。使用该方法,我们研究了H2受体阻滞剂法莫替丁(YM-11170)对水浸应激诱导的大鼠胃黏膜PG水平变化的影响。还估计了胃黏膜磷脂酶(PLase)活性。在胃黏膜中检测到四种PG,即6-酮-PGF1a、PGE2、PGF2a和PGD2。6小时水浸应激导致它们全部以相似程度下降,下降幅度约为对照值的70%。在应激6小时的大鼠中也观察到PLase活性下降。法莫替丁预处理可防止已知具有细胞保护作用的PG水平下降,并维持PLase活性。这些结果表明,法莫替丁通过维持PG水平和PLase活性发挥其抗溃疡作用。