Protection by the calcium antagonist Wy-47,037 against stress ulceration in the rat.
Wy-47,037, a novel compound with both intracellular and extracellular calcium-blocking properties, was evaluated for its effects on cold/restraint stress induced ulceration in the rat. Wy-47,037 dose-dependently inhibited ulcerogenesis; with an ED50 of 8 mg/kg, PO, it was approximately twice as potent as nitrendipine (ED50 = 15 mg/kg). Wy-47,037 also reduced basal gastric acid secretion (ED50 = 7 mg/kg) and gastrointestinal motility (ED50 = 16 mg/kg). It is thus possible that Wy-47,037's alteration of basal gastric acid secretion and/or of gastrointestinal motility may contribute to its therapeutic efficacy against stress induced ulcer formation.
Nielsen
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Department of Experimental Therapeutics, Wyeth Laboratories, Inc., Philadelphia, PA 19101.
Sulkowski
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D000818:Animals; D002121:Calcium Channel Blockers / Q000494:pharmacology*; D003080:Cold Temperature; D005744:Gastric Acid / Q000378:metabolism; D005769:Gastrointestinal Motility / Q000187:drug effects; D008297:Male; D009568:Nitrendipine / Q000494:pharmacology; D009930:Organic Chemicals; D011708:Pylorus / Q000502:physiology; D051381:Rats; D012149:Restraint, Physical; D013276:Stomach Ulcer / Q000209:etiology / Q000517:prevention & control*; D013315:Stress, Psychological / Q000150:complications / Q000503:physiopathology
D002121:Calcium Channel Blockers; D009930:Organic Chemicals; C055381:Wy 47037; D009568:Nitrendipine