SOLUBILIZATION OF HIGH-AFFINITY DOPAMINE RECEPTORS
SOLUBILIZATION OF HIGH-AFFINITY DOPAMINE RECEPTORS
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DOI：
10.1038/279072a0
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发表时间：
1979-01-01
期刊：
影响因子：
64.8
通讯作者：
LADURON, P
中科院分区：
文献类型：
--
作者：
GORISSEN, H;LADURON, P
神经兴奋药物被认为是通过阻断脑多巴胺受体发挥作用1。使用3 H-氟哌啶醇2，3或3 H-螺哌隆4，5进行的体外结合试验为这种相互作用提供了更直接的证据。尽管据报道螺哌隆在体外4 - 9和体内条件下5、10、11均可标记额叶皮质6、大鼠纹状体中的多巴胺能受体，但该药物的结合特征为多巴胺能。我们的实验室最近进行了溶解神经安定剂受体的初步尝试，但从毛地黄皂苷处理后的大鼠纹状体膜中获得的3 H-螺哌隆大分子复合物12除螺哌隆本身外，没有显示出与多巴胺激动剂和拮抗剂的原始高亲和力结合特征。最近，在小牛尾状核的毛地黄皂苷提取物中发现了溶解的神经抑制剂位点，但它们仍然没有被表征13。我们现在报告的溶解结合位点从狗纹状体保留膜结合多巴胺受体的特性。
NEUROLEPTIC drugs are thought to act by blocking brain dopamine receptors1.In vitrobinding assays using either3H-haloperidol2,3or3H-spiperone4,5have provided more direct evidence of this interaction. Although spiperone has been reported to label serotonergic receptors in the frontal cortex6, in the rat striatum, in bothin vitro4–9andin vivoconditions5,10,11, the binding characteristics of this drug are dopaminergic. Initial attempts to solubilise the neuroleptic receptor were recently undertaken in our laboratory, but the3H-spiperone macromolecular complex obtained from rat striatal membranes after digitonin treatment12did not show the original highaffinity binding characteristics for dopamine agonists and antagonists except for spiperone itself. More recently, solubilised neuroleptic sites were found in digitonin extracts from calf caudate but they were still not characterised13. We now report the solubilisation of binding sites from dog striatum which retain the characteristics of membrane-bound dopamine receptors.