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δ阿片受体镇痛:药理学和分子方法的最新贡献

Delta opioid receptor analgesia: recent contributions from pharmacology and molecular approaches.

作者信息

Gavériaux-Ruff Claire, Kieffer Brigitte Lina

机构信息

Institut de Génétique et de Biologie Moléculaire et Cellulaire, Université de Strasbourg, Centre National de la Recherche Scientifique, Institut National de la Santé et de la Recherche Médicale, Illkirch, France.

出版信息

Behav Pharmacol. 2011 Sep;22(5-6):405-14. doi: 10.1097/FBP.0b013e32834a1f2c.

Abstract

Delta opioid receptors represent a promising target for the development of novel analgesics. A number of tools have been developed recently that have significantly improved our knowledge of δ receptor function in pain control. These include several novel δ agonists with potent analgesic properties, and genetic mouse models with targeted mutations in the δ opioid receptor gene. Also, recent findings have further documented the regulation of δ receptor function at cellular level, which impacts on the pain-reducing activity of the receptor. These regulatory mechanisms occur at transcriptional and post-translational levels, along agonist-induced receptor activation, signaling and trafficking, or in interaction with other receptors and neuromodulatory systems. All these tools for in-vivo research, and proposed mechanisms at molecular level, have tremendously increased our understanding of δ receptor physiology, and contribute to designing innovative strategies for the treatment of chronic pain and other diseases such as mood disorders.

摘要

δ阿片受体是开发新型镇痛药的一个有前景的靶点。最近已经开发出了一些工具,这些工具显著增进了我们对δ受体在疼痛控制中功能的了解。其中包括几种具有强效镇痛特性的新型δ激动剂,以及δ阿片受体基因发生靶向突变的基因工程小鼠模型。此外,最近的研究结果进一步证明了δ受体功能在细胞水平上的调节,这会影响该受体的止痛活性。这些调节机制发生在转录和翻译后水平,涉及激动剂诱导的受体激活、信号传导和转运,或者与其他受体和神经调节系统的相互作用。所有这些用于体内研究的工具以及在分子水平上提出的机制,极大地增进了我们对δ受体生理学的理解,并有助于设计治疗慢性疼痛和其他疾病(如情绪障碍)的创新策略。

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The delta opioid receptor: an evolving target for the treatment of brain disorders.德尔塔阿片受体:治疗脑部疾病的新兴靶点。
Trends Pharmacol Sci. 2011 Oct;32(10):581-90. doi: 10.1016/j.tips.2011.06.008. Epub 2011 Sep 17.
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