Department of Chemistry and Chemical Biology, Harvard University, 12 Oxford St, Cambridge, MA 02138, United States of America.
Department of Chemistry and Chemical Biology, Harvard University, 12 Oxford St, Cambridge, MA 02138, United States of America.
Mol Cell Neurosci. 2023 Jun;125:103845. doi: 10.1016/j.mcn.2023.103845. Epub 2023 Mar 21.
The opioids are potent and widely used pain management medicines despite also possessing severe liabilities that have fueled the opioid crisis. The pharmacological properties of the opioids primarily derive from agonism or antagonism of the opioid receptors, but additional effects may arise from specific compounds, opioid receptors, or independent targets. The study of the opioids, their receptors, and the development of remediation strategies has benefitted from derivatization of the opioids as chemical tools. While these studies have primarily focused on the opioids in the context of the opioid receptors, these chemical tools may also play a role in delineating mechanisms that are independent of the opioid receptors. In this review, we describe recent advances in the development and applications of opioid derivatives as chemical tools and highlight opportunities for the future.
尽管阿片类药物具有严重的副作用，已经引发了阿片类药物危机，但它们仍然是一种有效的、广泛使用的止痛药物。阿片类药物的药理学特性主要源于对阿片受体的激动或拮抗作用，但特定化合物、阿片受体或独立靶点也可能产生额外的作用。阿片类药物、其受体的研究以及补救策略的发展都得益于阿片类药物作为化学工具的衍生化。虽然这些研究主要集中在阿片类药物与阿片受体的关系上，但这些化学工具也可能在阐明与阿片受体无关的机制方面发挥作用。在这篇综述中，我们描述了作为化学工具的阿片类药物衍生物的最新进展和应用，并强调了未来的机会。
