Mennini T, Garattini S
Institut de Recherches Pharmacologiques, Mario Negri, Milan, Italie.
Presse Med. 1991 Nov 14;20(37):1823-7.
In ex vivo experiments, tianeptine increased serotonin uptake in the hippocampus and the cortex acutely and after 72 hours following chronic administration for 15 days. This effect results from an increased maximal rate of uptake without changes in the number or affinity to binding sites for I'3H-imipramine or I'3H-paroxetin. In addition, tianeptine increased extracellular levels of 5-hydroxyindolacetic acid (5-HIAA) in hippocampus and hypothalamus measured with in vivo voltametry. It can thus be concluded that tianeptine also raises 5-hydrotryptamine (5HT) uptake in vivo. The effects of tianeptine on the serotoninergic system, especially the increase in serotonin uptake, are discussed in relation with its effects on behaviour and the dopaminergic and cholinergic systems.
在离体实验中,天丙替林在急性给药时以及在连续15天慢性给药72小时后,均可增加海马体和皮质中的5-羟色胺摄取。这种效应是由于摄取的最大速率增加,而对³H-丙咪嗪或³H-帕罗西汀结合位点的数量或亲和力没有变化。此外,通过体内伏安法测量,天丙替林可增加海马体和下丘脑中5-羟吲哚乙酸(5-HIAA)的细胞外水平。因此可以得出结论,天丙替林在体内也可提高5-羟色胺(5HT)的摄取。天丙替林对5-羟色胺能系统的影响,尤其是5-羟色胺摄取的增加,与其对行为以及多巴胺能和胆碱能系统的影响相关联进行了讨论。