Kuhn F J, Schingnitz G, Lehr E, Montagna E, Hinzen H D, Giachetti A
Department of Pharmacology, Boehringer Ingelheim KG, Ingelheim/Rhein, F.R.G.
Arch Int Pharmacodyn Ther. 1988 Mar-Apr;292:13-34.
The pharmacological effects of the novel compound WEB 1881 FU (4-amino-methyl-1-benzyl-pyrrolidine-2-one-fumarate) were investigated. The tests performed indicate that the compound has cytoprotective as well as metabolism and cognition enhancing and central cholinomimetic properties. The nootropic effects in all tests were more pronounced than those of piracetam, while the central cholinomimetic effects were generally weaker than those of directly acting cholinomimetic agents. However, the typical peripheral cholinergic side effects were not observed. From the results we believe that the stimulating effect of WEB 1881 FU upon the central cholinergic system is modulatory rather than direct. The combination of nootropic and cholinomimetic properties appears favorable for treatment of brain dysfunction in the elderly. Side effects are less serious than with other known cholinomimetics.
对新型化合物WEB 1881 FU(4-氨基甲基-1-苄基吡咯烷-2-酮富马酸盐)的药理作用进行了研究。所进行的试验表明,该化合物具有细胞保护作用以及增强代谢和认知的作用,还具有中枢拟胆碱特性。在所有试验中,其益智作用比吡拉西坦更显著,而中枢拟胆碱作用通常比直接作用的拟胆碱剂弱。然而,未观察到典型的外周胆碱能副作用。根据这些结果,我们认为WEB 1881 FU对中枢胆碱能系统的刺激作用是调节性的而非直接作用。益智特性与拟胆碱特性的结合似乎有利于治疗老年人的脑功能障碍。其副作用比其他已知的拟胆碱剂轻。