Abstract
We report here the design, synthesis, and in vitro characterization of new opioid peptides featuring a 4-anilidopiperidine moiety. Despite the fact that the chemical structures of fentanyl surrogates have been found suboptimal per se for the opioid activity, the corresponding conjugates with opioid peptides displayed potent opioid activity. These studies shed an instructive light on the strategies and potential therapeutic values of anchoring the 4-anilidopiperidine scaffold to different classes of opioid peptides.
Copyright © 2013 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
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Animals
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Cell Line
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Fentanyl / chemistry
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Humans
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Kinetics
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Mice
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Opioid Peptides / chemical synthesis
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Opioid Peptides / chemistry*
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Opioid Peptides / metabolism
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Piperidines / chemical synthesis
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Piperidines / chemistry*
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Piperidines / metabolism
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Protein Binding
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Receptors, Opioid, delta / chemistry
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Receptors, Opioid, delta / genetics
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Receptors, Opioid, delta / metabolism
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Receptors, Opioid, mu / chemistry
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Receptors, Opioid, mu / genetics
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Receptors, Opioid, mu / metabolism
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Structure-Activity Relationship
Substances
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Opioid Peptides
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Piperidines
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Receptors, Opioid, delta
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Receptors, Opioid, mu
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Fentanyl