Effects of the novel histamine H2-receptor antagonist (+/-)-(E)-1-[2-hydroxy-2-(4-hydroxyphenyl)ethyl]-3-[2-[[[5- (methylamino)methyl-2-furyl]methyl]thio]ethyl]-2-(methylsulfonyl) guanidine on gastric secretion and gastroduodenal ulcers in rats.

The effects of (+/-)-(E)-1-[2-hydroxy-2-(4-hydroxyphenyl)ethyl]-3-[2- [[[5-(methylamino)methyl-2-furyl] methyl]thio]ethyl]-2-(methylsulfonyl)guanidine (CAS 140695-21-2, T-593), a new histamine H2-receptor antagonist, on gastric secretion and experimental gastric and duodenal lesion/ulcer models in rats were examined. The drug administered orally or intraduodenally significantly and dose-dependently inhibited both basal and histamine-stimulated acid secretion. Pepsin output was also inhibited by the drug nearly dose-dependently. The acid-inhibitory effect of T-593 persisted for 12 h after a single oral administration. T-593 potently protected the gastric mucosa against water-immersion stress-, indometacin- and HCl.acetylsalicylic acid-induced lesions, but it had no effect on HCl.ethanol-induced lesions. T-593 significantly prevented the development of mepirizole-induced duodenal ulcers. Spontaneous healing of kissing gastric ulcers was significantly enhanced when T-593 was administered for 14 days. The antisecretory and antilesion/antiulcer effects of T-593 were similar to those of ranitidine and omeprazole. It is concluded that T-593 is a potent antisecretory and antiulcer drug.