[H-3] CITALOPRAM BINDING TO BRAIN AND PLATELET MEMBRANES OF HUMAN AND RAT
[H-3] CITALOPRAM BINDING TO BRAIN AND PLATELET MEMBRANES OF HUMAN AND RAT
复制标题
DOI：
10.1111/j.1471-4159.1991.tb02588.x
复制
发表时间：
1991-01-01
影响因子：
4.7
通讯作者：
MELLERUP, ET
中科院分区：
文献类型：
--
作者：
PLENGE, P;MELLERUP, ET
西酞普兰是一种选择性5-羟色胺（5-HT）摄取抑制剂，具有抗抑郁作用，可与人神经细胞膜和血小板膜上的5-HT转运蛋白高亲和力结合。 在20 ℃时，两种组织中的K（D）约为1.5 nM。 [H-3]西酞普兰与大鼠神经元膜的结合亲和力高于与人类神经元和血小板膜的结合亲和力;在20 ° C下，K（D）约为0.7 nM。[H-3]西酞普兰与血小板膜结合的B（max）值接近于使用5-HT摄取抑制剂[H-3]丙咪嗪和[H-3]帕罗西汀发现的值，表明所有三种5-HT摄取抑制剂均与5-HT转运蛋白结合。 在人和大鼠细胞膜中，[H-3]西酞普兰的解离速率随温度每升高4-5 ℃而增加两倍，尽管在任何给定温度下，人神经元和血小板细胞膜中的解离速率比大鼠神经元细胞膜中的解离速率快约4倍。
Citalopram, a selective serotonin (5-HT) uptake inhibitor with antidepressant properties, was found to bind with high affinity to the 5-HT transporter from human neuronal and platelet membranes. At 20-degrees-C, K(D) was about 1.5 nM in both tissues. [H-3]Citalopram bound to rat neuronal membranes with higher affinity than to human neuronal and platelet membranes; at 20-degrees-C K(D) was about 0.7 nM. The B(max) value for the binding of [H-3]citalopram to platelet membranes was close to that found using the 5-HT uptake inhibitors [H-3]imipramine and [H-3]paroxetine, suggesting that all three 5-HT uptake inhibitors bind to the 5-HT transporter. The dissociation rate of [H-3]citalopram increased twofold with each 4-5-degrees-C increase in temperature in both human and rat membranes, although at any given temperature, the dissociation rate was about four times faster in the human neuronal and platelet membranes than in rat neuronal membranes.