Mellerup E T, Plenge P
Psychopharmacology (Berl). 1986;89(4):436-9. doi: 10.1007/BF02412117.
Paroxetine is the most potent and one of the most specific serotonin uptake inhibitors. High-affinity 3H-paroxetine and 3H-imipramine binding was compared in rat neuronal membranes. The KD value for 3H-paroxetine binding to neuronal membranes was 0.08 nM, which is exactly the same value as with platelet membranes. The KD value for 3H-imipramine binding to neuronal membranes was about 4 nM, which is higher than the KD value for 3H-imipramine binding to platelet membranes (0.5 nM). The results indicated that the 3H-paroxetine binding site is identical in neuronal membranes and in platelet membranes; this binding site is probably located on the serotonin transport mechanism. In addition, part of the high-affinity 3H-imipramine binding to neuronal membranes is probably located on the serotonin transport mechanism, but another part is located elsewhere. Furthermore the polypeptides containing the 3H-imipramine binding sites may not be identical in neuronal and platelet membranes.
帕罗西汀是效力最强且最具特异性的5-羟色胺摄取抑制剂之一。对大鼠神经元膜中高亲和力的3H-帕罗西汀和3H-丙咪嗪结合进行了比较。3H-帕罗西汀与神经元膜结合的KD值为0.08 nM，这与血小板膜中的值完全相同。3H-丙咪嗪与神经元膜结合的KD值约为4 nM，高于3H-丙咪嗪与血小板膜结合的KD值（0.5 nM）。结果表明，3H-帕罗西汀结合位点在神经元膜和血小板膜中是相同的；该结合位点可能位于5-羟色胺转运机制上。此外，3H-丙咪嗪与神经元膜的部分高亲和力结合可能位于5-羟色胺转运机制上，但另一部分位于其他地方。此外，含有3H-丙咪嗪结合位点的多肽在神经元膜和血小板膜中可能并不相同。
