Sette M, Briley M S, Langer S Z
J Neurochem. 1983 Mar;40(3):622-8. doi: 10.1111/j.1471-4159.1983.tb08026.x.
Tricyclic antidepressant drugs inhibit [3H]imipramine binding to the rat brain cortex in a competitive manner, giving linear Hofstee plots and Hill coefficients of approximately 1.0. Serotonin, the only neurotransmitter to inhibit [3H]imipramine binding, does so in a complex manner, exhibiting a Hill coefficient of 0.40-0.50. Nontricyclic inhibitors of serotonin uptake such as fluoxetine, paroxetine, norzimelidine, and citalopram inhibit [3H]imipramine binding in the same complex manner as serotonin. These results are interpreted as suggesting that [3H]imipramine binds to a site associated with the serotonin uptake system but different from either the substrate recognition site for serotonin or the site of action of the nontricyclic inhibitors of neuronal uptake of serotonin.
三环类抗抑郁药物以竞争性方式抑制[3H]丙咪嗪与大鼠脑皮质的结合，得到线性霍夫斯蒂图，希尔系数约为1.0。血清素是唯一能抑制[3H]丙咪嗪结合的神经递质，其抑制方式复杂，希尔系数为0.40 - 0.50。血清素摄取的非三环类抑制剂，如氟西汀、帕罗西汀、去甲替林和西酞普兰，以与血清素相同的复杂方式抑制[3H]丙咪嗪结合。这些结果被解释为表明[3H]丙咪嗪与一个与血清素摄取系统相关的位点结合，但不同于血清素的底物识别位点或血清素神经元摄取的非三环类抑制剂的作用位点。
