Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy and Food Chemistry, Julius Maximilian University of Würzburg, 97074, Würzburg, Germany.
Chempluschem. 2020 Jun;85(6):1354-1364. doi: 10.1002/cplu.202000212.
Opioid receptors (ORs) are classified among the oldest and best investigated drug targets due to their fundamental role in the treatment of pain and related disorders. ORs are divided in three conventional subtypes (μ, κ, δ) and the non-classical nocicepetin receptor. All ORs are family A G protein-coupled receptors (GPCRs), and are located on the cell surface. Modern biophysical methods use light to investigate physiological processes at organismal, cellular and subcellular level. Many of these methods rely on fluorescent ligands, thus highlighting their importance. This review addresses the advancements in the development of opioid fluorescent ligands and their use in biological, pharmacological and imaging applications.
阿片受体（ORs）因其在治疗疼痛及相关疾病方面的基础性作用而被归为最古老和研究最透彻的药物靶点之一。ORs 分为三种传统亚型（μ、κ、δ）和非经典的 nocicepetin 受体。所有 ORs 都是家族 A G 蛋白偶联受体（GPCRs），位于细胞表面。现代生物物理方法利用光来研究生物体、细胞和亚细胞水平的生理过程。这些方法中有许多依赖于荧光配体，因此凸显了它们的重要性。本文综述了阿片类荧光配体的发展进展及其在生物学、药理学和成像应用中的应用。
