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天然DOR-MOR异聚体的证据及功能相关性

Evidence and Function Relevance of Native DOR-MOR Heteromers.

作者信息

Cahill Catherine M, Ong Edmund

机构信息

Department of Psychiatry and Biobehavioral Sciences, Hatos Center for Neuropharmacology, Semel Institute for Neuroscience and Human Behavior, University of California Los Angeles, Los Angeles, CA, USA.

Department of Anesthesiology, Duke University, Durham, NC, USA.

出版信息

Handb Exp Pharmacol. 2018;247:115-127. doi: 10.1007/164_2018_112.

Abstract

Opioid receptors are the sites of action for morphine and most other clinically used opioid drugs. Abundant evidence now demonstrates that different opioid receptor types can physically associate to form heteromers. Owing to their constituent monomers' involvement in analgesia, mu/delta opioid receptor (M/DOR) heteromers have been a particular focus of attention. Understandings of the physiological relevance and indisputable proof of M/DOR formation in vivo are still evolving. This aspect of the field has been slow to progress in large part by the limitations of most available experimental models; recently however, promising progress is being made. As a result, the long-repeated promise of opioid receptor heteromers as selective therapeutic targets is now being realized.

摘要

阿片受体是吗啡及大多数其他临床使用的阿片类药物的作用位点。现在有大量证据表明,不同类型的阿片受体可以物理结合形成异聚体。由于其组成单体参与镇痛作用,μ/δ阿片受体(M/DOR)异聚体一直是特别关注的焦点。对M/DOR在体内形成的生理相关性的理解以及确凿证据仍在不断发展。该领域的这一方面在很大程度上由于大多数现有实验模型的局限性而进展缓慢;然而最近正在取得有希望的进展。因此,阿片受体异聚体作为选择性治疗靶点长期以来反复被提及的前景现在正在实现。

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