Fluorescently labeled morphine derivatives for bioimaging studies
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 pri...
| Main Authors: | , , , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
American Chemical Society
2018
|
| Online Access: | https://eprints.nottingham.ac.uk/50021/ |
| _version_ | 1848798131303481344 |
|---|---|
| author | Lam, Raymond Gondin, Arisbel B. Canals, Meritxell Kellam, Barrie Briddon, Stephen J. Graham, Bim Scammells, Peter J. |
| author_facet | Lam, Raymond Gondin, Arisbel B. Canals, Meritxell Kellam, Barrie Briddon, Stephen J. Graham, Bim Scammells, Peter J. |
| author_sort | Lam, Raymond |
| building | Nottingham Research Data Repository |
| collection | Online Access |
| description | 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. |
| first_indexed | 2025-11-14T20:14:53Z |
| format | Article |
| id | nottingham-50021 |
| institution | University of Nottingham Malaysia Campus |
| institution_category | Local University |
| language | English |
| last_indexed | 2025-11-14T20:14:53Z |
| publishDate | 2018 |
| publisher | American Chemical Society |
| recordtype | eprints |
| repository_type | Digital Repository |
| spelling | nottingham-500212019-01-01T04:30:20Z https://eprints.nottingham.ac.uk/50021/ Fluorescently labeled morphine derivatives for bioimaging studies Lam, Raymond Gondin, Arisbel B. Canals, Meritxell Kellam, Barrie Briddon, Stephen J. Graham, Bim Scammells, Peter J. 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. American Chemical Society 2018-03-15 Article PeerReviewed application/pdf en https://eprints.nottingham.ac.uk/50021/1/2018%20JMedChem_Manuscript_Revised2.pdf 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 https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01811 doi:10.1021/acs.jmedchem.7b01811 doi:10.1021/acs.jmedchem.7b01811 |
| spellingShingle | Lam, Raymond Gondin, Arisbel B. Canals, Meritxell Kellam, Barrie Briddon, Stephen J. Graham, Bim Scammells, Peter J. Fluorescently labeled morphine derivatives for bioimaging studies |
| title | Fluorescently labeled morphine derivatives for bioimaging studies |
| title_full | Fluorescently labeled morphine derivatives for bioimaging studies |
| title_fullStr | Fluorescently labeled morphine derivatives for bioimaging studies |
| title_full_unstemmed | Fluorescently labeled morphine derivatives for bioimaging studies |
| title_short | Fluorescently labeled morphine derivatives for bioimaging studies |
| title_sort | fluorescently labeled morphine derivatives for bioimaging studies |
| url | https://eprints.nottingham.ac.uk/50021/ https://eprints.nottingham.ac.uk/50021/ https://eprints.nottingham.ac.uk/50021/ |