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ACP-103, a 5-HT2A/2C inverse agonist, potentiates haloperidol-induced dopamine release in rat medial prefrontal cortex and nucleus accumbens.ACP-103，一种5-羟色胺2A/2C反向激动剂，可增强氟哌啶醇诱导的大鼠内侧前额叶皮质和伏隔核中的多巴胺释放。
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Monoamine oxidase and catechol-o-methyltransferase enzyme activity and gene expression in response to sustained glucocorticoids.
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Induction patterns of transcription factors of the nur family (nurr1, nur77, and nor-1) by typical and atypical antipsychotics in the mouse brain: implication for their mechanism of action.典型和非典型抗精神病药物对小鼠大脑中核受体相关因子家族转录因子（Nurr1、Nur77和Nor-1）的诱导模式：对其作用机制的启示
J Pharmacol Exp Ther. 2005 Apr;313(1):460-73. doi: 10.1124/jpet.104.080184. Epub 2004 Dec 22.
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Dopamine reuptake by norepinephrine neurons: exception or rule?去甲肾上腺素能神经元对多巴胺的再摄取：是例外还是规律？
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Principles for modulation of the nuclear receptor superfamily.核受体超家族的调控原则。
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A transcriptional basis for physiology.生理学的转录基础。
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7
Docosahexaenoic acid reduces haloperidol-induced dyskinesias in mice: involvement of Nur77 and retinoid receptors.二十二碳六烯酸可减轻小鼠中氟哌啶醇诱导的运动障碍：Nur77和视黄酸受体的作用
Biol Psychiatry. 2004 Oct 1;56(7):522-6. doi: 10.1016/j.biopsych.2004.06.036.
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Tyrosine hydroxylase-positive neurons intrinsic to the human striatum express the transcription factor Nurr1.人类纹状体内的酪氨酸羟化酶阳性神经元表达转录因子Nurr1。
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The catechol-O-methyltransferase polymorphism: relations to the tonic-phasic dopamine hypothesis and neuropsychiatric phenotypes.儿茶酚-O-甲基转移酶基因多态性：与多巴胺紧张性-相位性假说及神经精神表型的关系
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Protein measurement with the Folin phenol reagent.使用福林酚试剂进行蛋白质测定。
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Nur77基因敲除会改变多巴胺能神经元的生化活性和多巴胺代谢。

Nur77 gene knockout alters dopamine neuron biochemical activity and dopamine turnover.

作者信息

Gilbert François, Morissette Marc, St-Hilaire Michel, Paquet Brigitte, Rouillard Claude, Di Paolo Thérèse, Lévesque Daniel

机构信息

Neuroscience Unit, CRCHUL and Faculty of Medicine, Laval University, Ste-Foy, Quebec, Canada.

出版信息

Biol Psychiatry. 2006 Sep 15;60(6):538-47. doi: 10.1016/j.biopsych.2006.04.023. Epub 2006 Aug 7.

DOI:10.1016/j.biopsych.2006.04.023
PMID:16893530
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5148625/
Abstract

BACKGROUND

Transcription factors of the Nur family (Nurr1, Nur77, and Nor-1) are orphan nuclear receptors closely associated with dopamine neurotransmission in the central nervous system. Nur77 expression is strongly modulated by antipsychotic and ant-parkinsonian drugs in dopaminoceptive brain areas. However, the role of Nur77 in dopamine neuron activity and turnover remains elusive.

METHODS

We compared various behavioral and biochemical parameters between Nur77 knockout -/- and wild-type +/+ mice in basal and haloperidol-challenged conditions.

RESULTS

We report here that Nur77-deficient mice display enhanced spontaneous locomotor activity, greater sensitivity to a small dose of the dopamine D2 receptor agonist quinpirole acting mainly at autoreceptor sites, and higher levels of the dopamine metabolite DOPAC relative to wild-type mice. Dopamine turnover disturbances are also found after acute challenge with haloperidol, a dopamine D2 receptor antagonist. These alterations are associated with increased tyrosine hydroxylase expression and activity, and reduced catechol-O-methyltransferase expression.

CONCLUSION

Taken together, these results are consistent with the involvement of Nur77 in dopamine neuron biochemical activity and dopamine turnover.

摘要

背景

Nur家族转录因子（Nurr1、Nur77和Nor-1）是孤儿核受体，与中枢神经系统中的多巴胺神经传递密切相关。在多巴胺感受性脑区，Nur77的表达受到抗精神病药物和抗帕金森病药物的强烈调节。然而，Nur77在多巴胺神经元活性和更新中的作用仍不清楚。

方法

我们比较了Nur77基因敲除-/-小鼠和野生型+/+小鼠在基础状态和氟哌啶醇激发条件下的各种行为和生化参数。

结果

我们在此报告，与野生型小鼠相比，Nur77基因缺陷小鼠表现出增强的自发运动活性、对主要作用于自身受体位点的小剂量多巴胺D2受体激动剂喹吡罗更敏感，以及多巴胺代谢产物3,4-二羟基苯乙酸（DOPAC）水平更高。在用多巴胺D2受体拮抗剂氟哌啶醇急性激发后，也发现了多巴胺更新紊乱。这些改变与酪氨酸羟化酶表达和活性增加以及儿茶酚-O-甲基转移酶表达降低有关。

结论

综上所述，这些结果与Nur77参与多巴胺神经元生化活性和多巴胺更新一致。