Gianni A M, Bruno G, Sirtori C
Institute of Pharmacology, University of Bologna, Italy.
Arzneimittelforschung. 1997 Nov;47(11A):1315-7.
In this study the efficacy of pivagabine (4-[(2,2-dimethyl-1-oxopropyl)amino]butanoic acid, CAS 69542-93-4, Tonerg) in preventing experimental stress ulcer in animals was evaluated. Twenty Wistar rats were randomly subdivided into 2 groups; one group received pivagabine (200 mg/kg orally) and the other tap water. The rats were immobilized in a cold room (2-4 degrees C) for 2 h, and the number and extension of gastric ulcerative and hemorrhagic lesions were evaluated. Pivagabine determined a significant reduction in the number of animals with gastric lesions (5 vs. 10, p < 0.05), in the linear extension of ulcers (2.0 +/- 0.8 vs. 7.2 +/- 1.7 mm, percent protection 72.2, p < 0.05) and in the linear extension of hemorrhages (2.6 +/- 1.0 vs. 10.3 +/- 1.6 mm, percent protection 74.8, p < 0.01). The protective effect of pivagabine on experimental stress-induced ulcers is likely to be mediated by the inhibition of corticotropin releasing factor release from hypothalamus, as also suggested by behavioral studies.
在本研究中，评估了吡戊加滨（4-[(2,2-二甲基-1-氧代丙基)氨基]丁酸，CAS 69542-93-4，Tonerg）对预防动物实验性应激性溃疡的疗效。将20只Wistar大鼠随机分为2组；一组给予吡戊加滨（口服200mg/kg），另一组给予自来水。将大鼠固定在冷室（2-4℃）中2小时，评估胃溃疡性和出血性病变的数量及范围。吡戊加滨使有胃部病变的动物数量显著减少（5只对10只，p<0.05），溃疡的线性范围缩小（2.0±0.8对7.2±1.7mm，保护率72.2%，p<0.05），出血的线性范围也缩小（2.6±1.0对10.3±1.6mm，保护率74.8%，p<0.01）。行为学研究也表明，吡戊加滨对实验性应激诱导溃疡的保护作用可能是通过抑制下丘脑促肾上腺皮质激素释放因子的释放来介导的。
