Department of Synthesis and Chemical Technology of Pharmaceutical Substances with Computer Modelling Lab, Medical University of Lublin, Lublin, Poland.
Curr Top Med Chem. 2020;20(31):2852-2865. doi: 10.2174/1568026620666200601155451.
Opioid signaling plays a central role in pain perception. As such, it remains the main target in the development of antinociceptive agents, despite serious side effects involved. In recent years, hopes for improved opioid painkillers are rising, together with our understanding of allosterism and biased signaling mechanisms. In this review, we focus on recently discovered allosteric modulators of opioid receptors, insights into phenomena underlying their action, as well as on how they extend our understanding of mechanisms of previously known compounds. A brief overlook of their synthesis is also presented.
阿片类信号在疼痛感知中起着核心作用。因此，尽管存在严重的副作用，但它仍然是开发抗伤害性药物的主要目标。近年来，人们对改善阿片类止痛药的希望与我们对变构作用和偏向信号传导机制的理解一起增加。在这篇综述中，我们专注于最近发现的阿片受体变构调节剂，深入了解它们作用的现象，以及它们如何扩展我们对以前已知化合物机制的理解。还简要介绍了它们的合成。
