Abstract
The noncationizable tripeptide Ac-D-Trp-Phe-GlyNH2 was recently proposed as a novel minimal recognition motif for μ-opioid receptor. The introduction of different substituents (methyl, halogens, nitro, etc.) at the indole of D-Trp significantly influenced receptor affinities and resulted in serum stability and in a measurable effect on central antinociception in mice after ip administration.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Analgesics, Opioid / metabolism*
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Animals
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HEK293 Cells
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Humans
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Indoles / chemical synthesis
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Indoles / chemistry*
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Indoles / pharmacology
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Mice
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Molecular Docking Simulation
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Oligopeptides / chemical synthesis
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Oligopeptides / chemistry*
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Oligopeptides / pharmacology
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Pain Measurement
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Protein Conformation
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Radioligand Assay
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Receptors, Opioid, delta / agonists
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Receptors, Opioid, delta / metabolism
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Receptors, Opioid, kappa / agonists
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Receptors, Opioid, kappa / metabolism
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Receptors, Opioid, mu / agonists
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Receptors, Opioid, mu / metabolism
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Structure-Activity Relationship
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Tryptophan / analogs & derivatives*
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Tryptophan / chemical synthesis
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Tryptophan / chemistry*
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Tryptophan / pharmacology
Substances
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Analgesics, Opioid
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Indoles
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Oligopeptides
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Receptors, Opioid, delta
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Receptors, Opioid, kappa
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Receptors, Opioid, mu
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Tryptophan