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Fluorescently Labeled Morphine Derivatives for Bioimaging Studies

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

Authors

Raymond Lam

Arisbel B. Gondin

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BARRIE KELLAM BARRIE.KELLAM@NOTTINGHAM.AC.UK
Professor of Medicinal Chemistry

Bim Graham

Peter J. Scammells



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 Mar 29, 2024
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