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Issue 7, 2019
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Affinity of fentanyl and its derivatives for the σ1-receptor

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Abstract

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.

Graphical abstract: Affinity of fentanyl and its derivatives for the σ1-receptor

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Article information


Submitted
16 Apr 2019
Accepted
18 May 2019
First published
13 Jun 2019

Med. Chem. Commun., 2019,10, 1187-1191
Article type
Research Article

Affinity of fentanyl and its derivatives for the σ1-receptor

P. F. J. Lipiński, E. Szűcs, M. Jarończyk, P. Kosson, S. Benyhe, A. Misicka, J. Cz. Dobrowolski and J. Sadlej, Med. Chem. Commun., 2019, 10, 1187
DOI: 10.1039/C9MD00222G

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