[Effect of lafutidine, a novel antiulcer agent, on healing and relapse of acetic acid-induced gastric ulcer in rats].
Effect of lafutidine ((+/-)-2-(furfurylsulfinyl)-N-[4-[4-(piperidinomethyl)-2-pyr idyl] oxy-(Z)-2-butenyl] acetamide, FRG-8813), a novel antiulcer agent, on the healing and relapse in acetic acid-induced gastric ulcer in rats was investigated. Lafutidine at 1, 3 or 10 mg/kg, twice daily for 10 days reduced the ulcer area in a dose-dependent manner, and the effect by 10 mg/kg of lafutidine was significant. The effect of famotidine at 1 mg/kg and cimetidine at 30 mg/kg, which have almost equal antisecretory activity to lafutidine at 10 mg/kg, on the ulcer area was not significant. Effect on the healing and relapse was assessed by endoscopy for 25 weeks after the induction of gastric ulcer. Drugs were administered twice daily for 11 weeks. Lafutidine at 3 mg/kg and famotidine at 1 mg/kg accelerated the healing, but cimetidine at 30 mg/kg did not. Cumulative relapse rate and inflammatory cell infiltration were significantly reduced in rats initially treated with lafutidine. Famotidine and cimetidine had no effect. In conclusion, lafutidine accelerated ulcer healing and prevented ulcer relapse in rats.
Onodera
S
S
Pharmaceuticals Research Laboratories, Fujirebio, Inc., Tokyo, Japan.
Tanaka
M
M
Aoyama
M
M
Arai
Y
Y
Shibata
M
M
Yamaura
T
T
Ohnishi
H
H
D000081:Acetamides / Q000008:administration & dosage / Q000627:therapeutic use*; D019342:Acetic Acid; D000818:Animals; D000897:Anti-Ulcer Agents / Q000627:therapeutic use*; D002927:Cimetidine / Q000627:therapeutic use; D004305:Dose-Response Relationship, Drug; D015738:Famotidine / Q000627:therapeutic use; D006635:Histamine H2 Antagonists / Q000627:therapeutic use*; D008297:Male; D010880:Piperidines / Q000008:administration & dosage / Q000627:therapeutic use*; D011725:Pyridines / Q000008:administration & dosage / Q000627:therapeutic use*; D051381:Rats; D017207:Rats, Sprague-Dawley; D012008:Recurrence; D013276:Stomach Ulcer / Q000139:chemically induced / Q000188:drug therapy* / Q000473:pathology
D000081:Acetamides; D000897:Anti-Ulcer Agents; D006635:Histamine H2 Antagonists; D010880:Piperidines; D011725:Pyridines; C076948:lafutidine; D015738:Famotidine; D002927:Cimetidine; D019342:Acetic Acid