@article{ChristianSeierDrakopoulosetal.2020,
  author    = {Christian, Gentzsch and Seier, Kerstin and Drakopoulos, Antonios and Jobin, Marie-Lise and Lanoisel{\´e}e, Yann and Koszegi, Zsombor and Maurel, Damien and Sounier, R{\´e}my and H{\"u}bner, Harald and Gmeiner, Peter and Granier, S{\´e}bastien and Calebiro, Davide and Decker, Michael},
  title     = {Selective and Wash-Resistant Fluorescent Dihydrocodeinone Derivatives Allow Single-Molecule Imaging of μ-Opioid Receptor Dimerization},
  series = {Angewandte Chemie International Edition},
  volume    = {59},
  journal   = {Angewandte Chemie International Edition},
  number    = {15},
  doi       = {10.1002/anie.201912683},
  url       = {http://nbn-resolving.de/urn:nbn:de:bvb:20-opus-212398},
  pages     = {5958-5964},
  year      = {2020},
  abstract  = {μ-Opioid receptors (μ-ORs) play a critical role in the modulation of pain and mediate the effects of the most powerful analgesic drugs. Despite extensive efforts, it remains insufficiently understood how μ-ORs produce specific effects in living cells. We developed new fluorescent ligands based on the μ-OR antagonist E-p-nitrocinnamoylamino-dihydrocodeinone (CACO), that display high affinity, long residence time and pronounced selectivity. Using these ligands, we achieved single-molecule imaging of μ-ORs on the surface of living cells at physiological expression levels. Our results reveal a high heterogeneity in the diffusion of μ-ORs, with a relevant immobile fraction. Using a pair of fluorescent ligands of different color, we provide evidence that μ-ORs interact with each other to form short-lived homodimers on the plasma membrane. This approach provides a new strategy to investigate μ-OR pharmacology at single-molecule level.},
  language  = {en}
}