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[3H]美舒麦角,一种5-羟色胺-2受体的选择性配体。

[3H]Mesulergine, a selective ligand for serotonin-2 receptors.

作者信息

Closse A

出版信息

Life Sci. 1983 May 23;32(21):2485-95. doi: 10.1016/0024-3205(83)90375-2.

Abstract

[3H]Mesulergine binds with high affinity to rat cerebral cortex membranes. (KD = 1.9 nM, Bmax = 11.3 pM/g tissue). The binding of this ligand is selective for serotonin-2 receptors: Its next highest affinity, which is for dopamine receptors labelled by neuroleptics, is about 50 times weaker than its affinity for serotonin-2 receptors. No significant affinity for serotonin-1, alpha 1-adrenergic or histamine H1 receptors was observed. Specific [3H]mesulergine binding was diminished in the presence of low concentrations of lithium ions.

摘要

[3H]美舒麦角以高亲和力与大鼠大脑皮层膜结合。(解离常数KD = 1.9纳摩尔,最大结合容量Bmax = 11.3皮摩尔/克组织)。该配体的结合对5-羟色胺-2受体具有选择性:其对多巴胺受体(由抗精神病药物标记)的第二高亲和力比对5-羟色胺-2受体的亲和力弱约50倍。未观察到对5-羟色胺-1、α1-肾上腺素能或组胺H1受体有明显亲和力。在低浓度锂离子存在下,特异性[3H]美舒麦角结合减少。

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