Affinity of fentanyl and its derivatives for the σ1-receptor.

@article{Lipiski2019AffinityOF,
  title={Affinity of fentanyl and its derivatives for the σ1-receptor.},
  author={Piotr F. J. Lipiński and E. Szűcs and Małgorzata Jarończyk and P. Kosson and S. Benyhe and A. Misicka and J. Dobrowolski and Joanna Sadlej},
  journal={MedChemComm},
  year={2019},
  volume={10 7},
  pages={
          1187-1191
        }
}
  • Piotr F. J. Lipiński, E. Szűcs, +5 authors Joanna Sadlej
  • Published 2019
  • Chemistry, Medicine
  • MedChemComm
  • Fentanyl and its 11 commercially available derivatives were investigated as to their affinity for the σ1 receptor. The parent compound is a rather poor binder (IC50 = 4973 nM), but its close derivatives (benzylfentanyl or p-fluorofentanyl) have submicromolar affinities. Modelling provides a structural basis for the observed trends in activity. 

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