Delta opioid receptor analgesia: recent contributions from pharmacology and molecular approaches.
Delta opioid receptor analgesia: recent contributions from pharmacology and molecular approaches.
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DOI：
10.1097/fbp.0b013e32834a1f2c
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发表时间：
2011-09
影响因子：
1.6
通讯作者：
Kieffer BL
中科院分区：
文献类型：
--
作者：
Gavériaux-Ruff C;Kieffer BL
δ阿片受体是开发新型镇痛药的一个很有前途的靶点。最近已经开发了许多工具，这些工具显着提高了我们对δ受体在疼痛控制中的功能的认识。这些包括几种具有强效镇痛特性的新型δ激动剂，以及在δ阿片受体基因中具有靶向突变的遗传小鼠模型。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，这影响了受体的镇痛活性。这些调节机制发生在转录和翻译后水平，沿着激动剂诱导的受体活化、信号传导和运输，或与其他受体和神经调节系统相互作用。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，极大地增加了我们对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。
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 delta receptor function in pain control. These include several novel delta agonists with potent analgesic properties, as well as genetic mouse models with targeted mutations in the delta opioid receptor gene. Also, recent findings have further documented the regulation of delta 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, as well as proposed mechanisms at molecular level, have tremendously increased our understanding of delta receptor physiology, and contribute to designing innovative strategies for the treatment of chronic pain and other diseases such as mood disorders.