Moret C, Briley M
J Neurochem. 1986 Nov;47(5):1609-13. doi: 10.1111/j.1471-4159.1986.tb00802.x.
In the rat hypothalamus [3H]imipramine binding is inhibited by tricyclic and nontricyclic antidepressant drugs in a complex manner, with biphasic curves and Hill coefficients less than 1.0. 5-Hydroxytryptamine (serotonin) inhibited with high affinity a decreasing proportion of the [3H]imipramine binding sites as the [3H]imipramine concentration was raised. In the absence of sodium ions, IC50 values for the inhibition by tricyclic and nontricyclic antidepressants were increased by approximately 1,000-fold, and the inhibition curves became classically monophasic with Hill coefficients close to 1.0. These data are interpreted as suggesting that [3H]imipramine binds to two independent sites in the rat hypothalamus. One site is sodium-dependent with a high affinity for the drugs tested; the other is sodium-independent and has a low affinity for these drugs.
在大鼠下丘脑，[3H]丙咪嗪结合受到三环和非三环抗抑郁药物的复杂抑制，呈现双相曲线且希尔系数小于1.0。随着[3H]丙咪嗪浓度升高，5-羟色胺（血清素）以高亲和力抑制的[3H]丙咪嗪结合位点比例逐渐降低。在无钠离子存在时，三环和非三环抗抑郁药抑制的IC50值增加约1000倍，抑制曲线变为典型的单相，希尔系数接近1.0。这些数据被解释为表明[3H]丙咪嗪在大鼠下丘脑与两个独立位点结合。一个位点依赖钠离子，对所测试药物具有高亲和力；另一个位点不依赖钠离子，对这些药物具有低亲和力。
