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 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.