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

J Med Chem. 2002 Dec 19;45(26):5617-9. doi: 10.1021/jm025575g.

Abstract

Arodyn (aromatic dynorphin) is a novel analogue of the opioid peptide dynorphin A with a nonbasic N-terminus that exhibits nanomolar affinity (K(i) = 10 nM) and remarkable selectivity for kappa opioid receptors (K(i) ratio (kappa/mu/delta) = 1/174/583). Arodyn completely reverses the agonism of dynorphin A (1-13)NH(2) in a concentration-dependent manner in the adenylyl cyclase assay. Thus arodyn is a novel kappa opioid receptor selective antagonist that will be useful to study these receptors.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Adenylyl Cyclases / metabolism
  • Amino Acid Sequence
  • Animals
  • CHO Cells
  • Cricetinae
  • Dynorphins / chemical synthesis*
  • Dynorphins / chemistry
  • Dynorphins / pharmacology
  • Peptide Fragments / chemical synthesis*
  • Peptide Fragments / chemistry
  • Peptide Fragments / pharmacology
  • Radioligand Assay
  • Receptors, Opioid, kappa / antagonists & inhibitors*
  • Structure-Activity Relationship

Substances

  • Peptide Fragments
  • Receptors, Opioid, kappa
  • arodyn
  • Dynorphins
  • dynorphin (1-11)
  • Adenylyl Cyclases