Departments of Oral and Maxillofacial Surgery, Pharmacology, and Physiology, Center for Biomedical Neuroscience, University of Texas Health San Antonio, San Antonio, Texas
Mol Pharmacol. 2019 May;95(5):463-467. doi: 10.1124/mol.118.114637. Epub 2019 Feb 5.
Opioids serve a vital role in the current analgesic array of treatment options. They are useful in acute instances involving severe pain associated with trauma, surgery, and terminal diseases such as cancer. In the past three decades, multiple receptor isoforms and conformations have been reported throughout literature. Most of these studies conducted systemic analyses of opioid receptor function, often generalizing findings from receptor systems in central nervous tissue or exogenously expressing immortalized cell lines as common mechanisms throughout physiology. However, a culmination of innovative experimental data indicates that opioid receptor systems are differentially modulated depending on their anatomic expression profile. Importantly, opioid receptors expressed in the peripheral nervous system undergo regulation uncommon to similar receptors expressed in central nervous system tissues. This distinctive characteristic begs one to question whether peripheral opioid receptors maintain anatomically unique roles, and whether they may serve an analgesic advantage in providing pain relief without promoting addiction.
阿片类药物在当前的镇痛治疗方案中发挥着至关重要的作用。它们在涉及创伤、手术和癌症等终末期疾病的严重疼痛的急性情况下非常有用。在过去的三十年中，文献中报道了多种受体同工型和构象。这些研究大多对阿片受体功能进行了系统分析，通常将中枢神经系统组织中受体系统或永生细胞系的发现概括为整个生理学的常见机制。然而，一系列创新的实验数据表明，阿片受体系统的调节因解剖表达谱的不同而不同。重要的是，在外周神经系统中表达的阿片受体经历的调节与在中枢神经系统组织中表达的类似受体不同。这种独特的特征让人怀疑外周阿片受体是否保持解剖学上独特的作用，以及它们是否可能在外周发挥镇痛优势，在不促进成瘾的情况下提供疼痛缓解。
