BAY P 1455, a thiazolylaminobenzimidazole derivative with gastroprotective properties in the rat.
The antiulcer activity of BAY P 14551 a thiazolylaminobenzimidazole derivative, was evaluated in different experimental ulcer models and its antiulcer activity was compared to that of different reference drugs. The overall activity of the compound was equal to or more potent than that of reference antiulcer drugs, such as pirenzepine, cimetidine and carbenoxolone, but it was not as potent as rioprostil. The ED50 values (expressed as mumol/kg p.o.) were 68 (confidence limits: 51-91) for indomethacin-induced ulcers, 21 (confidence limits: 13-31) for stress-induced ulcers and 1260 mumol/kg p.o. (confidence limits: 412-3800) for ulcers induced by absolute ethanol. The compound had no activity against cysteamine-induced duodenal ulcers and lost its cytoprotective activity in adrenalectomised rats. Since inhibition of gastric acid secretion was seen, if at all, only with the higher doses, the gastro-protective action of BAY P 1455 seemed not to be due to an antisecretory effect, but more likely to a gastroprotective action as hypothesised for prostaglandins.
Grassi
A
A
Department of Pharmacology, Bayer Italia, Garbagnate M.se MI.
Ippen
J
J
Bruno
M
M
Thomas
G
G
D000315:Adrenalectomy; D000818:Animals; D000897:Anti-Ulcer Agents; D001562:Benzimidazoles / Q000494:pharmacology*; D002927:Cimetidine / Q000494:pharmacology; D003345:Corticosterone / Q000097:blood; D003543:Cysteamine; D004381:Duodenal Ulcer / Q000139:chemically induced / Q000517:prevention & control; D000431:Ethanol; D005260:Female; D005744:Gastric Acid / Q000378:metabolism; D007101:Immersion; D066298:In Vitro Techniques; D007213:Indomethacin; D008297:Male; D010890:Pirenzepine / Q000494:pharmacology; D011458:Prostaglandins E / Q000494:pharmacology; D011708:Pylorus / Q000601:surgery; D051381:Rats; D011919:Rats, Inbred Strains; D016630:Rioprostil; D013276:Stomach Ulcer / Q000209:etiology / Q000517:prevention & control; D013315:Stress, Psychological / Q000150:complications; D013844:Thiazoles / Q000494:pharmacology*
D000897:Anti-Ulcer Agents; D001562:Benzimidazoles; D011458:Prostaglandins E; D013844:Thiazoles; C070344:2-(2'-benzimidazolyl)amino-4-methylthiazole; D010890:Pirenzepine; D000431:Ethanol; D003543:Cysteamine; D016630:Rioprostil; D002927:Cimetidine; D003345:Corticosterone; D007213:Indomethacin