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使用[3H]司来吉兰标记牛尾状核中的多巴胺能和5-羟色胺能受体。

Use of [3H]spiperone for labelling dopaminergic and serotonergic receptors in bovine caudate nucleus.

作者信息

Withy R M, Mayer R J, Strange P G

出版信息

J Neurochem. 1981 Nov;37(5):1144-54. doi: 10.1111/j.1471-4159.1981.tb04664.x.

DOI:10.1111/j.1471-4159.1981.tb04664.x
PMID:7299393
Abstract

[3H]Spiperone binding has been used to study neurotransmitter receptors in bovine caudate nucleus in displacement and saturation binding experiments. Displacement curves for several antagonists are biphasic and can be analysed into contributions from dopaminergic and serotonergic sites. Antagonist binding at each class of sites follows the simple mass action equations for binding at a homogeneous set of sites (slope factors close to unity). Agonist displacement curves also indicate complex behaviour, but agonist binding to the dopaminergic sites alone exhibits heterogeneous properties (slope factors less than unity). Saturation binding experiments have been conducted on each class of site, defining dopaminergic binding of [3H]spiperone as that binding displaced by 0.1 mM-dopamine and serotonergic binding as that displaced by 0.3 microM-mianserin. In each case, a single class of binding sites was detected: the binding parameters derived in this way have been used to calculate the proportions of the two classes of binding site observed in displacement experiments. Good agreement was obtained between calculated and observe values.

摘要

[3H]螺哌隆结合已被用于在置换和饱和结合实验中研究牛尾状核中的神经递质受体。几种拮抗剂的置换曲线是双相的,并且可以分析出多巴胺能和5-羟色胺能位点的贡献。每类位点上的拮抗剂结合遵循在一组同质位点上结合的简单质量作用方程(斜率因子接近1)。激动剂置换曲线也表明存在复杂行为,但仅激动剂与多巴胺能位点的结合表现出异质性(斜率因子小于1)。已对每类位点进行了饱和结合实验,将[3H]螺哌隆的多巴胺能结合定义为被0.1 mM多巴胺置换的结合,将5-羟色胺能结合定义为被0.3 μM米安色林置换的结合。在每种情况下,都检测到一类结合位点:以这种方式得出的结合参数已用于计算在置换实验中观察到的两类结合位点的比例。计算值与观察值之间取得了良好的一致性。

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J Neurochem. 1981 Nov;37(5):1144-54. doi: 10.1111/j.1471-4159.1981.tb04664.x.
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Functional coupling of the human dopamine D2 receptor with G alpha i1, G alpha i2, G alpha i3 and G alpha o G proteins: evidence for agonist regulation of G protein selectivity.人类多巴胺D2受体与Gαi1、Gαi2、Gαi3和Gαo G蛋白的功能偶联:激动剂对G蛋白选择性调节的证据。
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Spiperone: evidence for uptake into secretory granules.
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