Birnbaum J E, Wilson D E, Partridge R, Scruggs W, Sloboda A E, Mourillon S
Prostaglandins. 1981 Dec;22(6):957-70. doi: 10.1016/0090-6980(81)90024-1.
The effects of a new analogue of PGE1 (CL115,574) on gastric acid secretion, mucus secretion and protection against stress and indomethacin-induced ulcers were studied in the rat. CL115,574 was more potent than PGE1 and cimetidine in inhibiting acid secretion. CL115,574 protected against the development of stress and indomethacin-induced ulcers and prevented the indomethacin-induced decrease in hematocrit at an ED50 (3 micrograms/kg) far below the antisecretory ED50 (1 microgram/kg). While inhibiting acid secretion, CL115,574 increased the volume of gastric secretion indicating a stimulation of nonparietal cell secretion by the rat stomach. In addition the compound stimulated the secretion of mucus into the gastric juice. On the basis of its potency as an inhibitor of acid secretion and these additional effects which are indicative of cytoprotective activity, CL115,574 should be further studied as a possible anti-ulcer agent in man.
在大鼠中研究了一种新型前列腺素E1类似物（CL115,574）对胃酸分泌、黏液分泌以及对应激和吲哚美辛诱导溃疡的保护作用。CL115,574在抑制胃酸分泌方面比前列腺素E1和西咪替丁更有效。CL115,574可预防应激和吲哚美辛诱导溃疡的发生，并在远低于抗分泌半数有效剂量（1微克/千克）的半数有效剂量（3微克/千克）时防止吲哚美辛诱导的血细胞比容降低。在抑制胃酸分泌的同时，CL115,574增加了胃分泌量，表明其刺激了大鼠胃非壁细胞的分泌。此外，该化合物还刺激了黏液向胃液中的分泌。基于其作为胃酸分泌抑制剂的效力以及这些表明具有细胞保护活性的额外作用，CL115,574应作为一种可能的抗溃疡药物在人体中进行进一步研究。
