Affinity of fentanyl and its derivatives for the σ<sub>1</sub>-receptor.

Basic Information

ID: ALA4373662

Journal: Medchemcomm

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

Authors: Lipiński PFJ, Szűcs E, Jarończyk M, Kosson P, Benyhe S, Misicka A, Dobrowolski JC, Sadlej J.

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.

CiteXplore: 31391893

DOI: 10.1039/C9MD00222G

Patent ID: ┄

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