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

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.

SUBMITTER: Lipinski PFJ 

PROVIDER: S-EPMC6657672 | biostudies-literature | 2019 Jul

REPOSITORIES: biostudies-literature