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[Effects of 3-hydroxymethyl-2-methylimidazo [2, 1-b] benzothiazole (NIK-228) on gastric acid secretion and various experimental peptic ulcers in rats].

Abstract
We examined the antisecretory and antiulcer activities of NIK-228 in rats. Male Wistar rats (200 to 250 g) were used under 24 to 48 hr fasted (without water) conditions. NIK-228 and famotidine were administered orally 1 hr before pylorus ligation, stress or each ulceration inducer. Both NIK-228 (10 to 100 mg/kg) and famotidine (0.3 to 3 mg/kg) dose-dependently inhibited gastric secretion in pylorus ligated rats. Water-immersion stress-, indomethacin- or pylorus ligation (Shay)-induced gastric ulcers were dose-dependently inhibited by NIK-228 (10 to 100 mg/kg), but only water-immersion stress and indomethacin induced ulcers were dose-dependently inhibited by famotidine (0.03 to 3 mg/kg). Ethanol- and 0.6 N HCl-induced gastric lesions were remarkably inhibited by NIK-228 (ED50 = 2.7 and 5.6 mg/kg), but tended to be inhibited also by famotidine (0.3 to 3 mg/kg). Cysteamine-induced duodenal ulcer was inhibited significantly by NIK-228 (30, 100 mg/kg) or famotidine (3 mg/kg). NIK-228 may produce its antiulcer effects via antisecretory and cytoprotective effects. These results suggest that NIK-228 has antisecretory and antiulcer activities.
AuthorsR Hoshino, M Kagoshima, H Shimada
JournalNihon yakurigaku zasshi. Folia pharmacologica Japonica (Nihon Yakurigaku Zasshi) Vol. 97 Issue 5 Pg. 287-96 (May 1991) ISSN: 0015-5691 [Print] Japan
PMID1879806 (Publication Type: Comparative Study, Journal Article)
Chemical References
  • Anti-Ulcer Agents
  • Benzothiazoles
  • Imidazoles
  • Thiazoles
  • NIK 228
  • Famotidine
Topics
  • Administration, Oral
  • Animals
  • Anti-Ulcer Agents
  • Benzothiazoles
  • Depression, Chemical
  • Dose-Response Relationship, Drug
  • Famotidine (administration & dosage, pharmacology, therapeutic use)
  • Gastric Acid (metabolism)
  • Imidazoles (administration & dosage, pharmacology, therapeutic use)
  • Male
  • Peptic Ulcer (prevention & control)
  • Rats
  • Rats, Inbred Strains
  • Thiazoles (administration & dosage, pharmacology, therapeutic use)

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