[Cytoprotective activity of tiquizium bromide (HSR-902) and its mechanism]

Nihon Yakurigaku Zasshi. 1987 Nov;90(5):285-93. doi: 10.1254/fpj.90.285.
[Article in Japanese]

Abstract

The effects of HSR-902, an antimuscarinic agent, on acute gastric mucosal lesions induced by various necrotizing agents, gastric mucus secretion and gastric HCO3- secretion in rats were compared with those of pirenzepine.2HCl (pirenzepine), an antiulcer agent. 1) HSR-902 (10-100 mg/kg), given orally, dose-dependently prevented the gastric mucosal lesions induced by ethanol-HCl (60% ethanol in 150 mM HCl), aspirin-HCl (150 mg/kg of aspirin in 150 mM HCl), 0.6 N HCl and 0.2 N NaOH; and the cytoprotective effects of HSR-902 were almost equal or somewhat more potent than those of pirenzepine. 2) HSR-902 (30 mg/kg, p.o.), like pirenzepine, increased the alcian blue binding to gastric mucosa and both hexosamine and N-acetylneuramic acid in gastric juice and reversed the decrease of alcian blue binding to gastric mucosa in water-immersion stress. 3) HSR-902 (30 mg/kg, p.o.), unlike pirenzepine and atropine sulfate, increased the gastric HCO3- secretion in the pylorus-ligated preparations. 4) The cytoprotective effect of HSR-902 (30 mg/kg, p.o.), when examined using gastric mucosal lesion induced by aspirin-HCl, was not abolished by the pretreatment with indomethacin (10 mg/kg, s.c.) or N-ethylmaleimide (10 mg/kg, s.c.). 5) HSR-902 (30 mg/kg, p.o.) did not influence the gastric mucosal potential difference. These results suggest that HSR-902 is a promising drug for the treatment of gastritis and peptic ulcers.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Bicarbonates / metabolism
  • Ganglionic Blockers / pharmacology*
  • Ganglionic Blockers / therapeutic use
  • Gastric Mucosa / metabolism
  • Gastric Mucosa / pathology*
  • Male
  • Pirenzepine / pharmacology
  • Quinolizines / pharmacology*
  • Quinolizines / therapeutic use
  • Rats
  • Rats, Inbred Strains
  • Stomach Ulcer / drug therapy*

Substances

  • Bicarbonates
  • Ganglionic Blockers
  • Quinolizines
  • Pirenzepine
  • thiaton