title: Cytoprotective effects of NC-1300 and omeprazole on Hcl . ethanol-induced gastric lesions in rats.
abstract: NC-1300 (10-100 mg/kg), given p.o. at 0.5, 6, 12 or 24 hr before HCl . ethanol, dose-dependently protected the rat gastric mucosa. This protection was observed even when the gastric contents had been removed before application of HCl . ethanol. NC-1300 (30 mg/kg), given i.p., was without effect on lesion formation in a dose which potently inhibited gastric acid secretion in pylorus-ligated rats. pretreatment with indomethacin (5 mg/kg, s.c.) resulted in no reduction in the protection by NC-1300, excluding the possible participation of endogenous prostaglandins in the protective mechanism. N-ethylmaleimide pretreatment (10 mg/kg, s.c.) slightly reduced the protective activity of NC-1300, suggesting the partial participation of endogenous sulfhydryl compounds in the NC-1300 protection. NC-1300 sulfide and mercaptobenzimidazole (compounds obtained after mixing NC-1300 with acidic solution) also dose-dependently protected against HCl . ethanol-induced lesions when given p.o. at 0.5 hr before HCl . ethanol. The protection was significant but was considerably reduced in contrast to NC-1300 when the compounds were given 12 hr beforehand. NC-1300 sulfone had no effect on lesion formation. Omeprazole (10, 30 mg/kg), given p.o., also dose-dependently inhibited HCl . ethanol-induced lesions. However, the duration of protection was shorter than that seen with NC-1300, i.e., the effect disappeared 12 hr later. Thus, NC-1300 has a potent and long-lasting activity on HCl . ethanol-induced gastric lesions. The mechanism by which this occurs remains unknown.
mesh_terms: D053799:2-Pyridinylmethylsulfinylbenzimidazoles; D000818:Animals; D000897:Anti-Ulcer Agents; D001562:Benzimidazoles / Q000494:pharmacology*; D000431:Ethanol; D005033:Ethylmaleimide / Q000494:pharmacology; D005750:Gastric Juice / Q000378:metabolism; D005753:Gastric Mucosa / Q000187:drug effects / Q000473:pathology; D006851:Hydrochloric Acid; D007213:Indomethacin / Q000494:pharmacology; D008297:Male; D009853:Omeprazole / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D013276:Stomach Ulcer / Q000139:chemically induced / Q000517:prevention & control*; D013450:Sulfones / Q000494:pharmacology
chemical_list: D053799:2-Pyridinylmethylsulfinylbenzimidazoles; D000897:Anti-Ulcer Agents; D001562:Benzimidazoles; D013450:Sulfones; C048733:2-((2-dimethylaminobenzyl)sulfinyl)benzimidazole; D000431:Ethanol; C030698:2-mercaptobenzimidazole; D009853:Omeprazole; D005033:Ethylmaleimide; D006851:Hydrochloric Acid; D007213:Indomethacin