Antiulcer and gastric secretory activity of N-phthaloyl gamma-aminobutyric acid

Eur J Pharmacol. 1992 Aug 25;219(2):211-5. doi: 10.1016/0014-2999(92)90298-i.

Abstract

N-Phthaloyl gamma-aminobutyric acid, a new gamma-aminobutyric acid derivative synthesized in this laboratory, has been found to possess anticonvulsant, antinociceptive and antistress activities. Effects of this derivative on gastric lesions induced by aspirin and ethanol were studied in rats. N-Phthaloyl gamma-aminobutyric acid significantly inhibited both aspirin and alcohol ulceration. The ED50 in each case being 76.34 and 43.65 mg/kg i.p. respectively. The volume of gastric acid secretion was diminished but gastric mucus secretion was significantly enhanced. The antiulcer effect was blocked by bicuculline and 3-mercaptopropionic acid. We conclude that (a) N-phthaloyl gamma-aminobutyric acid possesses antiulcer activity (b) the new derivative is probably a non-specific gamma-aminobutyric acid receptor agonist (c) the observed activity may be due to a mucoprotective action.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 3-Mercaptopropionic Acid / pharmacology
  • Animals
  • Anti-Ulcer Agents / pharmacology*
  • Anti-Ulcer Agents / therapeutic use
  • Aspirin / toxicity
  • Bicuculline / pharmacology
  • Ethanol / toxicity
  • Gastric Acid / metabolism*
  • Mucus / metabolism*
  • Rats
  • Rats, Wistar
  • Stomach Ulcer / chemically induced
  • Stomach Ulcer / drug therapy*
  • gamma-Aminobutyric Acid / analogs & derivatives*
  • gamma-Aminobutyric Acid / pharmacology
  • gamma-Aminobutyric Acid / therapeutic use

Substances

  • Anti-Ulcer Agents
  • N-phthaloyl-4-aminobutyric acid
  • Ethanol
  • gamma-Aminobutyric Acid
  • 3-Mercaptopropionic Acid
  • Aspirin
  • Bicuculline