Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 61, Issue 3, Pages 1316-1329Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.7b01811
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Funding
- Australian Government Research Training Program Scholarship
- Monash Nottingham Joint Doctoral Training Centre program
- Medical Research Council [MR/N020081/1]
- MRC [MR/N020081/1] Funding Source: UKRI
- Medical Research Council [MR/N020081/1] Funding Source: researchfish
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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 mu-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.
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