Effect of ebrotidine on ethanol-induced gastric mucosal damage in the rat. Comparative study with other H2-receptor antagonists.

Abstract

Ebrotidine (N-[(E)-[[2-[[[2-[(diaminomethylene)amino]-4-thiazolyl]methyl]thio]ethyl ] amino]methylene]-4-bromo-benzenesulfonamide, CAS 100981-43-9, FI-3542) is a novel H2-receptor antagonist with additional gastroprotective effect. The gastroprotective effect of oral doses of ebrotidine against ethanol-induced mucosal damage in female rats was compared with the effect of cimetidine, ranitidine and famotidine. Macroscopically, ebrotidine showed dose-dependent inhibition of the lesion, with significant differences from that of controls at doses of > or = 12.50 mg/kg (ED50 was 26.54 mg/kg). None of the other drugs tested showed gastroprotective effect under the same conditions. The histopathological study revealed significant reduction in the number of deep and superficial ulcers in ebrotidine-treated animals. The gastroprotective effect of ebrotidine is patent even in the presence of indometacin suggesting that prostaglandins play a rather negligible role in gastroprotective action. These results suggest that ebrotidine may be more useful than the classically known H2-antagonists in the treatment of peptic ulcers.

• Authors: D Palop, A Romero, F Villamayor, L Conejo, A Sacristán, J A Ortiz
• Journal: Arzneimittel-Forschung (Arzneimittelforschung) Vol. 47 Issue 4A Pg. 450-4 (Apr 1997) ISSN: 0004-4172 [Print] Germany
• PMID: 9205742 (Publication Type: Comparative Study, Journal Article)

Chemical References

• Benzenesulfonates
• Histamine H2 Antagonists
• Thiazoles
• Ethanol
• Famotidine
• Cimetidine
• Ranitidine
• ebrotidine
• Indomethacin

Topics

• Animals
• Benzenesulfonates (administration & dosage, pharmacology)
• Cimetidine (administration & dosage, pharmacology)
• Dose-Response Relationship, Drug
• Ethanol (adverse effects)
• Famotidine (administration & dosage, pharmacology)
• Female
• Gastric Mucosa (drug effects, pathology)
• Histamine H2 Antagonists (administration & dosage, pharmacology)
• Indomethacin (pharmacology)
• Peptic Ulcer (chemically induced, prevention & control)
• Ranitidine (administration & dosage, pharmacology)
• Rats
• Rats, Sprague-Dawley
• Thiazoles (administration & dosage, pharmacology)