Development and Biological Applications of Fluorescent Opioid Ligands

Chempluschem. 2020 Jun;85(6):1354-1364. doi: 10.1002/cplu.202000212.

Abstract

Opioid receptors (ORs) are classified among the oldest and best investigated drug targets due to their fundamental role in the treatment of pain and related disorders. ORs are divided in three conventional subtypes (μ, κ, δ) and the non-classical nocicepetin receptor. All ORs are family A G protein-coupled receptors (GPCRs), and are located on the cell surface. Modern biophysical methods use light to investigate physiological processes at organismal, cellular and subcellular level. Many of these methods rely on fluorescent ligands, thus highlighting their importance. This review addresses the advancements in the development of opioid fluorescent ligands and their use in biological, pharmacological and imaging applications.

Keywords: biophysics; fluorescent ligands; imaging; microscopy; opioid receptors.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Fluorescent Dyes / chemistry*
  • Humans
  • Ligands
  • Microscopy, Confocal
  • Microscopy, Fluorescence
  • Neoplasms / diagnostic imaging
  • Neoplasms / metabolism
  • Receptors, Opioid, delta / metabolism*
  • Receptors, Opioid, kappa / metabolism*
  • Receptors, Opioid, mu / metabolism*

Substances

  • Fluorescent Dyes
  • Ligands
  • Receptors, Opioid, delta
  • Receptors, Opioid, kappa
  • Receptors, Opioid, mu