Effect of the 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 acute gastric mucosal injury in rats and its free-radical scavenging activities

Arzneimittelforschung. 1997 Jul;47(7):845-8.

Abstract

The protective effect of T-593 ((+/-)-(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), a new histamine H2-receptor antagonist, was investigated in rats with acute gastric mucosal injury. An ischemic injury followed by reperfusion was produced by applying a small vascular clamp to the celiac artery for 30 min and then removing it for 60 min. T-593 significantly reduced the area of the lesion in the stomach in a dose-dependent manner, and doses of 0.3 and 3.0 mg/kg inhibited the increase of lipid peroxides in the gastric mucosa after ischemia-reperfusion. A spin-trapping method using 5,5-dimethyl-1-pyrroline-N-oxide showed that T-593 scavenged hydroxyl radicals generated by the hydrogen peroxide-ferrous iron sulfate system. T-593 also significantly inhibited the increase of lipid peroxides induced by free-radical initiators in gastric mucosal homogenates. Thus, the protective effect of T-593 against acute gastric mucosal injury induced by ischemia and followed by reperfusion may result, in part, from its antioxidant properties.

MeSH terms

  • Animals
  • Anti-Ulcer Agents / pharmacology*
  • Anti-Ulcer Agents / therapeutic use
  • Free Radical Scavengers / pharmacology*
  • Free Radical Scavengers / therapeutic use
  • Gastric Mucosa / blood supply
  • Gastric Mucosa / pathology*
  • Guanidines / pharmacology*
  • Guanidines / therapeutic use
  • Histamine H2 Antagonists / pharmacology*
  • Histamine H2 Antagonists / therapeutic use
  • Hydroxyl Radical
  • Lipid Peroxides / blood
  • Lipid Peroxides / metabolism
  • Male
  • Rats
  • Rats, Sprague-Dawley
  • Regional Blood Flow / drug effects
  • Reperfusion Injury / pathology
  • Stomach Ulcer / pathology
  • Stomach Ulcer / prevention & control*
  • Sulfones / pharmacology*
  • Sulfones / therapeutic use
  • Superoxides / metabolism
  • Thiobarbituric Acid Reactive Substances / metabolism

Substances

  • Anti-Ulcer Agents
  • Free Radical Scavengers
  • Guanidines
  • Histamine H2 Antagonists
  • Lipid Peroxides
  • Sulfones
  • Thiobarbituric Acid Reactive Substances
  • Superoxides
  • T 593
  • Hydroxyl Radical