Anti-ulcer effect of 3-[p-(trans-4-aminomethylcyclohexylcarbonyl) phenyl] propionic acid hydrochloride (TEI-5103).
The anti-ulcer effects of the newly synthesized compound 3-[p-(trans-4-aminomethylcyclohexylcarbonyl)-phenyl]propionic acid hydrochloride (TEI-5103) on experimentally induced ulcers in rats were studied. TEI-5103 at doses of 25 to 400 mg/kg p.o. prevented formation of ulcers induced by serotonin, indomethacin, acetylsalicylic acid or stress (acute ulcer models), its effect being greater against gastric ulcers induced by serotonin. On acetic acid ulcer (chronic ulcer model), TEI-5103 at a daily dose of 200 mg/kg p.o. accelerated the healing of ulcers. TEI-5103 at doses of 100 to 400 mg/kg i.d. did not inhibit gastric acid secretion in pylorus-ligated rats. It markedly increased gastric blood flow in anesthetized rats (at 10-20 mg/kg i.v., measured by the aminopyrine clearance method), and also increased gastric blood flow in anesthetized dogs (at 2.5-10 mg/kg i.v., measured by the cross thermocouple method). These results indicate that TEI-5103 is effective as an anti-ulcer agent increasing gastric mucosal blood flow and possibly promoting the healing process of peptic ulcers.
D000085:Acetates; D019342:Acetic Acid; D000632:Aminopyrine / Q000378:metabolism; D000818:Animals; D000897:Anti-Ulcer Agents / Q000494:pharmacology*; D001241:Aspirin; D001626:Bethanechol Compounds / Q000494:pharmacology; D002927:Cimetidine / Q000494:pharmacology; D004285:Dogs; D005750:Gastric Juice / Q000378:metabolism; D005753:Gastric Mucosa / Q000098:blood supply; D006471:Gastrointestinal Hemorrhage / Q000517:prevention & control; D007213:Indomethacin; D008297:Male; D010666:Phenylpropionates / Q000494:pharmacology*; D011708:Pylorus / Q000502:physiology; D051381:Rats; D011919:Rats, Inbred Strains; D012039:Regional Blood Flow / Q000187:drug effects; D012701:Serotonin; D013276:Stomach Ulcer / Q000139:chemically induced; D013312:Stress, Physiological / Q000150:complications; D014148:Tranexamic Acid / Q000031:analogs & derivatives / Q000494:pharmacology
D000085:Acetates; D000897:Anti-Ulcer Agents; D001626:Bethanechol Compounds; D010666:Phenylpropionates; D000632:Aminopyrine; D012701:Serotonin; C000665:cetraxate; D014148:Tranexamic Acid; D002927:Cimetidine; C045302:TEI 5103; D019342:Acetic Acid; D001241:Aspirin; D007213:Indomethacin