Discovery of dermorphin-based affinity labels with subnanomolar affinity for mu opioid receptors

Bhaswati Sinha, Zhengyu Cao, Thomas F. Murray, Jane V. Aldrich

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Abstract

A series of potent electrophilic affinity labels (IC50= 0.1-5 nM) containing either a bromoacetamide or isothiocyanate based on the μ opioid receptor (MOR) selective peptide dermorphin were prepared. All four analogues exhibited wash resistant inhibition of [3H]DAMGO binding at subnanomolar to nanomolar concentrations, suggesting that these analogues bind covalently to MOR. To our knowledge, these peptides are the highest affinity peptide-based affinity labels for MOR reported to date.

Original languageEnglish
Pages (from-to)7372-7375
Number of pages4
JournalJournal of Medicinal Chemistry
Volume52
Issue number23
DOIs
Publication statusPublished - Dec 10 2009

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All Science Journal Classification (ASJC) codes

  • Molecular Medicine
  • Drug Discovery

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