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Affinity of fentanyl and its derivatives for the σ1-receptor
Piotr F J Lipiński1, Edina Szűcs2,3, Małgorzata Jarończyk4
1Department of Neuropeptides , Mossakowski Medical Research Centre , Polish Academy of Sciences , 02-106 Warsaw , Poland .
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.
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