Fluorescently Labeled Morphine Derivatives for Bioimaging Studies

Lam, Raymond; Gondin, Arisbel B.; Canals, Meritxell; Kellam, Barrie; Briddon, Stephen J.; Graham, Bim; Scammells, Peter J.

Abstract

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.

Citation

Lam, R., Gondin, A. B., Canals, M., Kellam, B., Briddon, S. J., Graham, B., & Scammells, P. J. (2018). Fluorescently Labeled Morphine Derivatives for Bioimaging Studies. Journal of Medicinal Chemistry, 61(3), 1316-1329. https://doi.org/10.1021/acs.jmedchem.7b01811

• Journal Article Type: Article
• Acceptance Date: Dec 30, 2017
• Online Publication Date: Jan 10, 2018
• Publication Date: Feb 8, 2018
• Deposit Date: Feb 26, 2018
• Publicly Available Date: Jan 11, 2019
• Journal: Journal of Medicinal Chemistry
• Print ISSN: 0022-2623
• Electronic ISSN: 1520-4804
• Publisher: American Chemical Society
• Peer Reviewed: Peer Reviewed
• Volume: 61
• Issue: 3
• Pages: 1316-1329
• DOI: https://doi.org/10.1021/acs.jmedchem.7b01811
• Public URL: https://nottingham-repository.worktribe.com/output/920401
• Publisher URL: https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01811
• Additional Information: This document is the Accepted Manuscript version of a Published Work that appeared in final form in Journal of Medicinal Chemistry, copyright ©2018 American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01811
• Contract Date: Feb 26, 2018