Fluorescently labeled morphine derivatives for bioimaging studies

Lam, Raymond, Gondin, Arisbel B., Canals, Meritxell, Kellam, Barrie, Briddon, Stephen J., Graham, Bim and Scammells, Peter J. (2018) Fluorescently labeled morphine derivatives for bioimaging studies. Journal of Medicinal Chemistry, 61 (3). pp. 1316-1329. ISSN 1520-4804

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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.

Item Type: Article
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
Schools/Departments: University of Nottingham, UK > Faculty of Medicine and Health Sciences > School of Life Sciences
University of Nottingham, UK > Faculty of Science > School of Pharmacy
Identification Number: 10.1021/acs.jmedchem.7b01811
Depositing User: Eprints, Support
Date Deposited: 26 Feb 2018 14:22
Last Modified: 01 Jan 2019 04:30
URI: https://eprints.nottingham.ac.uk/id/eprint/50021

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