Yoshikawa S, Ishitani R
Neuropharmacology. 1984 Oct;23(10):1227-30. doi: 10.1016/0028-3908(84)90245-4.
In synaptic membranes prepared from whole rat brain, cinanserin produced a relatively shallow inhibition curve of [3H] 5-HT binding with Hill slope of 0.68, as compared with that observed in the [3H]spiperone binding (Hill slope = 0.99). Furthermore, nonlinear regression analysis demonstrated that the former inhibition curve is best fitted by a two-site model. Regional and Scatchard analyses both clearly revealed that, in rat brain, at least two populations of binding sites were labelled by [3H]5-HT; however, high affinity binding sites (K(D) = 1.90 nM, Bmax = 0.188 pmoles/mg protein) could apparently be differentiated from the others by the action of 5 nM cinanserin.
在从整个大鼠脑制备的突触膜中，与在[3H] 螺哌隆结合中观察到的情况（希尔斜率 = 0.99）相比，辛那色林产生了一条相对较浅的[3H] 5-羟色胺结合抑制曲线，希尔斜率为0.68。此外，非线性回归分析表明，前一条抑制曲线最适合用双位点模型拟合。区域分析和斯卡查德分析均清楚地显示，在大鼠脑中，至少有两类结合位点被[3H] 5-羟色胺标记；然而，5 nM辛那色林的作用显然可以将高亲和力结合位点（解离常数KD = 1.90 nM，最大结合容量Bmax = 0.188皮摩尔/毫克蛋白质）与其他位点区分开来。
