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首页> 外文期刊>Life sciences >Inhibition of (3H)quinpirole binding by a monoamine oxidase inhibitor in subcellular fractions of rat striatum.
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Inhibition of (3H)quinpirole binding by a monoamine oxidase inhibitor in subcellular fractions of rat striatum.

机译：单胺氧化酶抑制剂抑制大鼠纹状体亚细胞部分中的（3H）喹吡罗结合。

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[3H]Quinpirole is a dopamine agonist with high affinity for D2-like dopamine receptors. A number of non-dopaminergic compounds, most notably monoamine oxidase inhibitors (MAOIs), inhibit the binding of [3H]quinpirole, but not other D2-like agonists and antagonists, in rat striatal membranes by a mechanism that does not involve the enzymatic activity of MAO. To further characterize this novel interaction, the subcellular distribution of spiperone-displaceable, "D2-like" [3H]quinpirole-labeled sites in rat striatum was assessed and compared with the distribution of MAOI-displaceable [3H]quinpirole binding (MQB). "D2-like" [3H]quinpirole binding exhibited similar nanomolar affinity in the crude synaptosomal (P2), crude microsomal (P3), and ribosomal, post-microsomal (P4) fractions. Total binding activity (fmol bound/fraction) of "D2-like" [3H]quinpirole binding was concentrated in the synaptosomal fraction (P2B). The subcellular distribution of MQB paralleled that of "D2-like" [3H]quinpirole binding. This suggests that "D2-like" [3H]quinpirole binding and MQB occur at a common membrane-bound binding site.
机译：[3H]喹吡罗是对D2样多巴胺受体具有高亲和力的多巴胺激动剂。许多非多巴胺能化合物，最主要的是单胺氧化酶抑制剂（MAOI），通过不涉及酶活性的机制抑制大鼠纹状体膜中[3H]喹吡罗的结合，但不抑制其他D2样激动剂和拮抗剂的结合。的。为了进一步表征这种新颖的相互作用，评估了大鼠纹状体中可替换为螺旋酮的，“ D2样” [3H]喹吡罗标记的位点的亚细胞分布，并将其与MAOI可替换[3H]喹吡罗结合（MQB）的分布进行了比较。 “ D2样” [3H]喹吡罗结合在粗突触体（P2），粗微粒体（P3）和核糖体，微粒体后（P4）组分中表现出相似的纳摩尔亲和力。 “ D2样” [3H]喹吡罗结合的总结合活性（fmol结合/部分）集中在突触体部分（P2B）中。 MQB的亚细胞分布与“ D2样” [3H]喹吡罗结合的平行。这表明“ D2样” [3H]喹吡罗结合和MQB发生在共同的膜结合结合位点。

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