Banerji S, Habibuddin M, Pal S P
Department of Pharmaceutical Technology, Jadavpur University, Calcutta, India.
Eur J Pharmacol. 1992 Aug 25;219(2):211-5. doi: 10.1016/0014-2999(92)90298-i.
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.
N-邻苯二甲酰基γ-氨基丁酸是本实验室合成的一种新型γ-氨基丁酸衍生物,已发现它具有抗惊厥、镇痛和抗应激活性。研究了该衍生物对阿司匹林和乙醇诱导的大鼠胃损伤的影响。N-邻苯二甲酰基γ-氨基丁酸显著抑制了阿司匹林和乙醇引起的溃疡。每种情况下的半数有效剂量分别为腹腔注射76.34和43.65毫克/千克。胃酸分泌量减少,但胃黏液分泌显著增加。荷包牡丹碱和3-巯基丙酸可阻断其抗溃疡作用。我们得出结论:(a)N-邻苯二甲酰基γ-氨基丁酸具有抗溃疡活性;(b)这种新衍生物可能是一种非特异性γ-氨基丁酸受体激动剂;(c)观察到的活性可能归因于黏膜保护作用。