Effects of the new histamine H2-receptor antagonist N-ethyl-N'-[3-[3-(piperidinomethyl)phenoxy]propyl] urea with potent gastric mucosal protective activity on acute gastric lesions and duodenal ulcers in rats

Arzneimittelforschung. 1993 Feb;43(2):134-8.

Abstract

The effects of KU-1257 (N-ethyl-N'-[3-[3-(piperidinomethyl)phenoxy]propyl]urea, CAS 120958-90-9) on gastric lesions and duodenal ulcers in rats were compared with those of various antiulcer drugs. KU-1257 prevented the formation of gastric lesions induced by necrotizing agents. The ID50 values against 0.6 N HCl-induced gastric lesions were 18.6 mg/kg, p.o. and 6.0 mg/kg, i.p. The ID50 values against absolute ethanol- and 1% NH3-induced gastric lesions were 12.4 and 9.2 mg/kg, p.o., respectively. Roxatidine acetate, troxipide and teprenone at doses of 100-200 mg/kg p.o. also significantly prevented the formation of gastric lesions by these necrotizing agents. Cimetidine, ranitidine and famotidine had no protective effect against these gastric lesions even at a dose of 200 mg/kg p.o. KU-1257, roxatidine acetate and famotidine inhibited acetylsalicylic acid- and water-immersion stress-induced gastric lesions. KU-1257, roxatidine acetate and famotidine inhibited mepirizole-induced duodenal ulcers, but not troxipide and teprenone. These results suggest that KU-1257 is more potent in the mucosal protective action than troxipide, teprenone, roxatidine acetate and other histamine H2-receptor antagonists.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Anti-Ulcer Agents / pharmacology*
  • Aspirin
  • Cyanides
  • Duodenal Ulcer / chemically induced
  • Duodenal Ulcer / pathology
  • Duodenal Ulcer / prevention & control*
  • Epirizole
  • Ethanol
  • Gastric Mucosa / drug effects*
  • Gastric Mucosa / pathology
  • Histamine H2 Antagonists / pharmacology*
  • Hydrochloric Acid
  • Immersion
  • Intestinal Mucosa / pathology
  • Male
  • Phenylurea Compounds / pharmacology*
  • Piperidines / pharmacology*
  • Rats
  • Rats, Wistar
  • Stomach Ulcer / chemically induced
  • Stomach Ulcer / pathology
  • Stomach Ulcer / prevention & control*
  • Stress, Psychological / complications

Substances

  • Anti-Ulcer Agents
  • Cyanides
  • Histamine H2 Antagonists
  • Phenylurea Compounds
  • Piperidines
  • KU 1257
  • Epirizole
  • Ethanol
  • Hydrochloric Acid
  • Aspirin