Quantitative determination of dopamine receptor subtypes not linked to activation of adenylate cyclase in rat striatum.
Quantitative determination of dopamine receptor subtypes not linked to activation of adenylate cyclase in rat striatum.
复制标题
定量测定与大鼠纹状体腺苷酸环化酶的激活无关的多巴胺受体亚型。
DOI：
10.1073/pnas.79.23.7561
复制
发表时间：
1982
影响因子：
11.1
通讯作者：
Molinoff,PB
中科院分区：
文献类型：
--
作者：
Huff,RM;Molinoff,PB
[3 H]多潘立酮和[3 H]螺哌啶的结合进行了检查，从大鼠纹状体制备的膜。[3 H]多潘立酮结合的Scatchard分析得到的曲线图与多种结合位点的存在一致。未转换数据的非线性回归分析表明，曲率是最好的解释由两个人口的结合位点的存在。Scatchard图的结合[3 H]螺哌啶是线性的，这表明该放射性配体结合到一个单一的类受体。然而，在抑制[3 H]spiroperidol结合的一些竞争配体的研究中获得的结果是不一致的，这些代理商与一个单一的类的结合位点的相互作用。计算机辅助分析的Hofstee图的6个竞争配体给出了相同的相对比例为两类网站确定的结合[3 H]多潘立酮的分析。用[3 H]螺哌啶标记的两类受体对多潘立酮的亲和力与[3 H]多潘立酮的两个结合位点群体的亲和力相似。此外，[3 H]螺哌利多的结合位点数等于[3 H]多潘立酮的结合位点总数。这些发现表明，这两个放射性配体结合到相同的两类结合位点。这两类纹状体部位都不可能是5-羟色胺的受体。所描述的方法将使得有可能评估生理或药理学操作对多巴胺受体亚型的密度或性质的影响。
The binding of [3H]domperidone and [3H]spiroperidol was examined in membranes prepared from rat striatum. Scatchard analysis of the binding of [3H]domperidone resulted in curvilinear plots consistent with the presence of multiple classes of binding sites. Nonlinear regression analysis of untransformed data showed that the curvature was best explained by the presence of two populations of binding sites. Scatchard plots of the binding of [3H]spiroperidol were linear, suggesting that this radioligand binds to a single class of receptors. However, results obtained in studies of the inhibition of [3H]spiroperidol binding by a number of competing ligands were not consistent with the interaction of these agents with a single class of binding sites. Computer-assisted analysis of the Hofstee plots of six competing ligands gave the same relative proportion for two classes of sites as determined by analysis of the binding of [3H]domperidone. The two classes of receptors labeled with [3H]spiroperidol had affinities for domperidone that were similar to those of the two populations of binding sites for [3H]domperidone. Furthermore, the number of binding sites for [3H]spiroperidol was equal to the total number of binding sites for [3H]domperidone. These findings suggest that the two radioligands bind to the same two classes of binding sites. It is unlikely that either of the two classes of striatal sites are receptors for serotonin. The approach described will make it possible to assess the effects of physiological or pharmacological manipulations on the densities or properties of subtypes of dopamine receptors.