Opioids, like morphine, are the mainstay analgesics for the treatment and control of pain. Despite this, they often exhibit severe side effects that limit dose; patients often become tolerant and dependent on these drugs, which remains a major health concern. The analgesic actions of opioids are primarily mediated via the μ-opioid receptor, a member of the G protein-coupled receptor superfamily. Thus far, development of small molecule fluorescent ligands for this receptor has resulted in antagonists, somewhat limiting the use of these probes. Herein, we describe our work on the development of a small molecule fluorescent probe based on the clinically used opiate morphine and initial characterization of its behavior in cell-based assays.

中文翻译：

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用于生物成像研究的荧光标记吗啡衍生物

阿片类药物（如吗啡）是用于治疗和控制疼痛的主要止痛药。尽管如此，它们经常表现出严重的副作用，限制了剂量。患者通常会变得耐受并依赖这些药物，这仍然是一个主要的健康问题。阿片类药物的镇痛作用主要通过μ阿片受体介导，该受体是G蛋白偶联受体超家族的成员。迄今为止，针对该受体的小分子荧光配体的开发已经产生了拮抗剂，从而在一定程度上限制了这些探针的使用。在这里，我们描述了基于临床使用的鸦片吗啡开发小分子荧光探针的工作，以及在基于细胞的测定中其行为的初步表征。