Whittle B J
Eur J Pharmacol. 1976 Dec;40(2):233-9. doi: 10.1016/0014-2999(76)90057-1.
The formation of gastric mucosal erosions induced by indomethacin in the rat was inhibited in a time- and dose-dependent manner by antisecretory prostaglandins, the methyl analogues of PGE2 being 400 times as active as the parent prostaglandin. PGA2, a methyl analogue of PGF2alpha and the H2-receptor antagonist metiamide, also inhibited erosion formation. There was a variable relationship between the doses required to inhibit erosions and to inhibit gastric acid secretion. In the anaesthetised rat, the low incidence of erosions with indomethacin was markedly increased by concurrent gastric perfusion with acid saline and taurocholate. This mucosal damage was inhibited by the methyl analogues of PGE2, suggesting protective actions on the mucosa other than inhibition of acid secretion.
消炎痛诱导的大鼠胃黏膜糜烂的形成,被抗分泌性前列腺素以时间和剂量依赖性方式抑制,PGE2的甲基类似物的活性是母体前列腺素的400倍。PGA2,一种PGF2α的甲基类似物以及H2受体拮抗剂甲硫米特,也抑制糜烂的形成。抑制糜烂所需剂量与抑制胃酸分泌所需剂量之间存在可变关系。在麻醉大鼠中,同时用酸性盐水和牛磺胆酸盐进行胃灌注,可使消炎痛引起的糜烂低发生率显著增加。这种黏膜损伤被PGE2的甲基类似物抑制,提示其对黏膜具有除抑制胃酸分泌之外的保护作用。