Fluorescently Labeled Morphine Derivatives for Bioimaging Studies

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

Research output: Contribution to journalArticleResearchpeer-review

Abstract

© 2018 American Chemical Society. 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.
Original languageEnglish
Pages (from-to)1316-1329
Number of pages14
JournalJournal of Medicinal Chemistry
Volume61
Issue number3
DOIs
Publication statusPublished - 8 Feb 2018

Cite this

Lam, Raymond ; Gondin, Arisbel B. ; Canals, Meritxell ; Kellam, Barrie ; Briddon, Stephen J. ; Graham, Bim ; Scammells, Peter J. / Fluorescently Labeled Morphine Derivatives for Bioimaging Studies. In: Journal of Medicinal Chemistry. 2018 ; Vol. 61, No. 3. pp. 1316-1329.
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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.

In: Journal of Medicinal Chemistry, Vol. 61, No. 3, 08.02.2018, p. 1316-1329.

Research output: Contribution to journalArticleResearchpeer-review

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AU - Canals, Meritxell

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AB - © 2018 American Chemical Society. 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.

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