Antiulcer activity of the calcium antagonist propyl-methylenedioxyindene--I. Effect on cold/restraint stress-induced ulcers in rats.

Abstract

1. Propyl-methylenedioxyindene (pr-MDI) is an intracellularly acting calcium antagonist with H2-receptor blocking properties. Stimulus-secretion coupling is inhibited by much lower concentrations of pr-MDI than is excitation-contraction coupling. 2. Since the processes leading to gastric ulceration are calcium-dependent, the aim of this study was to determine if pr-MDI could provide useful antiulcer activity at doses below those required to produce cardiovascular effects. 3. The antiulcer activity of pr-MDI (10-30 mg/kg) was examined in the cold (4 degree C)/restraint (3 hr) stress-induced ulcer model in male rats, and compared with the effects of the H2-blocker cimetidine (10-30 mg/kg) and the calcium channel blocker verapamil (11-32 mg/kg). The drugs were administered intraperitoneally 10 min prior to the cold/restraint stress. 4. All three drugs significantly reduced the number of ulcers and the cumulative length of ulcerated stomach surface in a roughly dose-dependent and equivalent manner. However, whereas the antiulcer doses of verapamil were extremely high, those of pr-MDI were one-sixth to one-half of its antiarrhythmic ED50 in rodents.

• Authors: W S Wong, R G Rahwan
• Journal: General pharmacology (Gen Pharmacol) Vol. 21 Issue 3 Pg. 321-5 ( 1990) ISSN: 0306-3623 [Print] England
• PMID: 2341019 (Publication Type: Journal Article)

Chemical References

• Anti-Ulcer Agents
• Indenes
• Cimetidine
• propylmethylenedioxyindene
• Verapamil

Topics

• Animals
• Anti-Ulcer Agents (pharmacology)
• Cimetidine (pharmacology)
• Cold Temperature
• Dose-Response Relationship, Drug
• Gastric Mucosa (pathology)
• Indenes (pharmacology)
• Male
• Rats
• Rats, Inbred Strains
• Restraint, Physical
• Stomach Ulcer (drug therapy, etiology, pathology)
• Stress, Physiological (complications)
• Verapamil (pharmacology)