Identification of arodyn, a novel acetylated dynorphin a-(1-11) analogue, as a κ opioid receptor antagonist

Marco A. Bennett, Thomas F. Murray, Jane V. Aldrich

Research output: Contribution to journalArticle

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Abstract

Arodyn (aromatic dynorphin) is a novel analogue of the opioid peptide dynorphin A with a nonbasic N-terminus that exhibits nanomolar affinity (Ki = 10 nM) and remarkable selectivity for κ opioid receptors (Ki ratio (κ/μ/δ) = 1/174/583). Arodyn completely reverses the agonism of dynorphin A (1-13)NH2 in a concentration-dependent manner in the adenylyl cyclase assay. Thus arodyn is a novel κ opioid receptor selective antagonist that will be useful to study these receptors.

Original languageEnglish (US)
Pages (from-to)5617-5619
Number of pages3
JournalJournal of Medicinal Chemistry
Volume45
Issue number26
DOIs
StatePublished - Dec 19 2002

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All Science Journal Classification (ASJC) codes

  • Molecular Medicine
  • Drug Discovery

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