Anti-ulcer effects of 4'-(2-carboxyetyl) phenyl trans-4-aminomethyl cyclohexanecarboxylate hydrochloride (cetraxate) on various experimental gastric ulcers in rats.
Anti-ulcer effects of cetraxate, a new compound possessing anti-plasmin, anti-casein and anti-trypsin actions were investigated by using experimental gastric ulcer models in rats. Cetraxate, 300 mg/kg p.o. showed significant inhibitory effects of 65.3%, 70.0%, 30.2%, and 67.1% against aucte types of ulcers producing by aspirin, phenylbutazone, indomethacin, and pyloric ligature (Shay's ulcer), respectively. These effects were greater than those obtained by gefarnate and aluminum sucrose sulfate may be mainly attributed to the protecting action of this drug on gastric mucosa. Ctraxate further revealed remarkable inhibitory effects on chronic types of ulcers produced by acetic acid, clamping, and clamping-cortisone. In acetic acid ulcer in particular, cetraxate was found to have a dose-dependent inhibitory effect at doses over 50 mg/kg. Of test drugs including L-glutamine and methylmethionine sulfonium chloride, cetraxate showed the most remarkable inhibitory effect on beta-glucuronidase activity in ulcer tissue of these three types of ulcers. These findings suggest that cetraxate may prevent the connective tissue in the ulcer location from decomposition due to lysosomal enzymes such as beta-glucuronidase, thereby accelerating the recovery from ulcer.
D000085:Acetates; D000818:Animals; D000897:Anti-Ulcer Agents; D001241:Aspirin; D003348:Cortisone; D003509:Cyclohexanecarboxylic Acids / Q000494:pharmacology* / Q000627:therapeutic use; D004195:Disease Models, Animal; D005260:Female; D005966:Glucuronidase / Q000037:antagonists & inhibitors; D007213:Indomethacin; D010653:Phenylbutazone; D011708:Pylorus / Q000502:physiology; D051381:Rats; D013276:Stomach Ulcer / Q000188:drug therapy* / Q000201:enzymology / Q000209:etiology
D000085:Acetates; D000897:Anti-Ulcer Agents; D003509:Cyclohexanecarboxylic Acids; D005966:Glucuronidase; D010653:Phenylbutazone; D001241:Aspirin; D003348:Cortisone; D007213:Indomethacin