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Title: 4-Phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives, a novel class of selective 6-opioid agonists
Authors: Trabanco, AA ×
Pullan, S
Alonso, JM
Alvarez, RM
Andres, JI
Boeckx, I
Fernandez, J
Gomez, A
Iturrino, L
Janssens, FE
Leenaerts, JE
De Lucas, AI
Matesanz, E
Meert, Theo
Steckler, T #
Issue Date: Jan-2006
Publisher: Pergamon-elsevier science ltd
Series Title: Bioorganic & medicinal chemistry letters vol:16 issue:1 pages:146-149
Abstract: A novel series of 4-phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives has been prepared and their synthesis described herein. In vitro affinities for delta-, mu-, and kappa-opioid receptors, as well as the functional activity in the [S-35]GTP gamma S assay are reported. The most potent and selective delta-opioid agonist 18a exhibited a K-i of 18 nM, and was > 258-fold and 28-fold selective over mu- and kappa-receptors, respectively; the compound is a full agonist with an EC50 value of 14 nM. (c) 2005 Elsevier Ltd. All rights reserved.
URI: 
ISSN: 0960-894X
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Non-KU Leuven Association publications
× corresponding author
# (joint) last author

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