Abstract
Derivatives of the delta opioid receptor selective peptide Tyr-Tic-Phe-Phe-OH (TIPP) containing a p-bromoacetamide moiety on the phenyl ring of Phe(3) or Phe(4) were prepared by solid phase synthesis. [Phe(p-NHCOCH(2)Br)(4)]TIPP exhibited high affinity for cloned delta receptors (IC(50) = 5.4 nM), and incubation with only 2.5 nM resulted in 85% wash resistant inhibition of radioligand binding to delta receptors. Therefore, this peptide is a potent affinity label for further study of delta opioid receptors.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Affinity Labels / chemical synthesis*
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Affinity Labels / chemistry
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Affinity Labels / pharmacology
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Animals
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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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Ligands
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Male
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Mice
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Oligopeptides / chemical synthesis*
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Oligopeptides / chemistry
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Oligopeptides / pharmacology
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Radioligand Assay
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Receptors, Opioid, delta / agonists
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Receptors, Opioid, delta / antagonists & inhibitors
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Receptors, Opioid, delta / drug effects*
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Tetrahydroisoquinolines*
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Vas Deferens / drug effects
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Vas Deferens / physiology
Substances
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Affinity Labels
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Ligands
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Oligopeptides
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Receptors, Opioid, delta
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Tetrahydroisoquinolines
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tyrosyl-1,2,3,4-tetrahydroisoquinoline-3-carbonyl-phenylalanyl-4-bromoacetamidophenylalanine