Abstract
A fluorescent tripeptide probe derived by coupling fluorescein to H-Dmt-Tic-Glu-NH2 was developed to interact with delta-opioid receptors with high affinity (Ki = 0.035 nM) and selectivity (Ki(mu)/Ki(delta) = 4371). It acts as an irreversible delta-opioid receptor antagonist, and binding to NG108-15 cells is blocked by the standard nonpeptidic delta-opioid receptor antagonist naltrindole. This probe should prove useful in the study of the distribution of delta-opioid receptors in tissues and the internalization of opioid peptides during signal transduction.
MeSH terms
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Animals
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Brain / metabolism
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Brain / ultrastructure
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Cell Line
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Dipeptides / chemistry*
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Electric Stimulation
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Fluorescent Dyes / chemical synthesis*
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Fluorescent Dyes / chemistry
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Fluorescent Dyes / pharmacology
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Guinea Pigs
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Ileum / drug effects
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Ileum / physiology
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In Vitro Techniques
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Male
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Mice
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Muscle Contraction / drug effects
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Muscle, Smooth / drug effects
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Muscle, Smooth / physiology
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Radioligand Assay
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Rats
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Receptors, Opioid, delta / antagonists & inhibitors*
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Synaptosomes / drug effects
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Synaptosomes / metabolism
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Tetrahydroisoquinolines / chemistry*
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Vas Deferens / drug effects
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Vas Deferens / physiology
Substances
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2',6'-dimethyltyrosyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid
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Dipeptides
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Fluorescent Dyes
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Receptors, Opioid, delta
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Tetrahydroisoquinolines