TY - JOUR
T1 - Fluorescently Labeled Morphine Derivatives for Bioimaging Studies
AU - Lam, Raymond
AU - Gondin, Arisbel B.
AU - Canals, Meritxell
AU - Kellam, Barrie
AU - Briddon, Stephen J.
AU - Graham, Bim
AU - Scammells, Peter J.
PY - 2018/2/8
Y1 - 2018/2/8
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=85041906089&partnerID=8YFLogxK
U2 - 10.1021/acs.jmedchem.7b01811
DO - 10.1021/acs.jmedchem.7b01811
M3 - Article
AN - SCOPUS:85041906089
SN - 0022-2623
VL - 61
SP - 1316
EP - 1329
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
IS - 3
ER -