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哺乳动物雷帕霉素靶蛋白(mTOR)激酶介导氟哌啶醇引起的僵住行为。

The mammalian target of rapamycin (mTOR) kinase mediates haloperidol-induced cataleptic behavior.

机构信息

Department of Neuroscience, The Scripps Research Institute, Florida, Jupiter, Florida, 33458, USA.

Department of Environmental, Biological, and Pharmaceutical Sciences and Technologies, University of Campania Luigi Vanvitelli, 81100, Caserta, Italy.

出版信息

Transl Psychiatry. 2020 Oct 2;10(1):336. doi: 10.1038/s41398-020-01014-x.

Abstract

The mammalian target of rapamycin (mTOR) is a ubiquitously expressed serine/threonine kinase protein complex (mTORC1 or mTORC2) that orchestrates diverse functions ranging from embryonic development to aging. However, its brain tissue-specific roles remain less explored. Here, we have identified that the depletion of the mTOR gene in the mice striatum completely prevented the extrapyramidal motor side effects (catalepsy) induced by the dopamine 2 receptor (D2R) antagonist haloperidol, which is the most widely used typical antipsychotic drug. Conversely, a lack of striatal mTOR in mice did not affect catalepsy triggered by the dopamine 1 receptor (D1R) antagonist SCH23390. Along with the lack of cataleptic effects, the administration of haloperidol in mTOR mutants failed to increase striatal phosphorylation levels of ribosomal protein pS6 (S235/236) as seen in control animals. To confirm the observations of the genetic approach, we used a pharmacological method and determined that the mTORC1 inhibitor rapamycin has a profound influence upon post-synaptic D2R-dependent functions. We consistently found that pretreatment with rapamycin entirely prevented (in a time-dependent manner) the haloperidol-induced catalepsy, and pS6K (T389) and pS6 (S235/236) signaling upregulation, in wild-type mice. Collectively, our data indicate that striatal mTORC1 blockade may offer therapeutic benefits with regard to the prevention of D2R-dependent extrapyramidal motor side effects of haloperidol in psychiatric illness.

摘要

哺乳动物雷帕霉素靶蛋白(mTOR)是一种广泛表达的丝氨酸/苏氨酸激酶蛋白复合物(mTORC1 或 mTORC2),它协调从胚胎发育到衰老的各种功能。然而,其在脑组织中的特定作用仍较少被探索。在这里,我们已经确定,在小鼠纹状体中耗尽 mTOR 基因完全阻止了多巴胺 2 受体(D2R)拮抗剂氟哌啶醇引起的锥体外系运动副作用(僵住),氟哌啶醇是最广泛使用的典型抗精神病药物。相反,小鼠纹状体中缺乏 mTOR 不会影响多巴胺 1 受体(D1R)拮抗剂 SCH23390 引起的僵住。伴随着僵住效应的缺乏,氟哌啶醇在 mTOR 突变体中的给药未能增加纹状体核糖体蛋白 pS6(S235/236)的磷酸化水平,就像在对照动物中看到的那样。为了证实遗传方法的观察结果,我们使用了一种药理学方法,并确定 mTORC1 抑制剂雷帕霉素对突触后 D2R 依赖性功能有深远的影响。我们一致发现,雷帕霉素预处理(以时间依赖性方式)完全阻止了氟哌啶醇诱导的僵住,以及 pS6K(T389)和 pS6(S235/236)信号转导的上调,在野生型小鼠中。总的来说,我们的数据表明,纹状体 mTORC1 阻断可能在预防精神病中氟哌啶醇依赖的 D2R 引起的锥体外系运动副作用方面提供治疗益处。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/79a3/7532208/49668225f91b/41398_2020_1014_Fig1_HTML.jpg

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