Abstract
New 4-anilidopiperidine analogues in which the phenethyl group of fentanyl was replaced by several aromatic ring-contained amino acids (or acids) were synthesized to study the biological effect of the substituents on mu and delta opioid receptor interactions. These analogues showed broad (47 nM-76 microM) but selective (up to 17-fold) binding affinities at the mu opioid receptor over the delta opioid receptor, as predicted from the message-address concept.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Analgesics / chemistry
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Analgesics / pharmacology
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Animals
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Cell Line
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Humans
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Ligands
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Molecular Structure
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Muscle Contraction / drug effects
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Piperidines / chemistry*
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Piperidines / pharmacokinetics*
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Protein Binding
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Receptors, Opioid, delta / drug effects
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Receptors, Opioid, delta / metabolism*
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Receptors, Opioid, mu / drug effects
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Receptors, Opioid, mu / metabolism*
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Structure-Activity Relationship
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Transfection
Substances
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Analgesics
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Ligands
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Piperidines
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Receptors, Opioid, delta
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Receptors, Opioid, mu