Affinity of fentanyl and its derivatives for the ?1-receptor.
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ABSTRACT:
SUBMITTER: Lipinski PFJ
PROVIDER: S-EPMC6657672 | biostudies-literature | 2019 Jul
REPOSITORIES: biostudies-literature
Publications
Affinity of fentanyl and its derivatives for the σ<sub>1</sub>-receptor.
Lipiński Piotr F J PFJ Szűcs Edina E Jarończyk Małgorzata M Kosson Piotr P Benyhe Sándor S Misicka Aleksandra A Dobrowolski Ján Cz JC Sadlej Joanna J
MedChemComm 20190613 7
Fentanyl and its 11 commercially available derivatives were investigated as to their affinity for the σ<sub>1</sub> receptor. The parent compound is a rather poor binder (IC<sub>50</sub> = 4973 nM), but its close derivatives (benzylfentanyl or <i>p</i>-fluorofentanyl) have submicromolar affinities. Modelling provides a structural basis for the observed trends in activity. ...[more]
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