Identification of Arodyn, a Novel Acetylated Dynorphin A-(1−11) Analogue, as a κ Opioid Receptor Antagonist

Citations Over Time

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.

Related Papers

• → NMR structure and dynamics of the agonist dynorphin peptide bound to the human kappa opioid receptor(2015)95 cited
• → Agonist and antagonist effects of dynorphin A-(1-13) in a thermal antinociception assay in rhesus monkeys.(1995)20 cited
• → In Major Depression, Increased Serum Dynorphin and Kappa Opioid Receptor Levels are Positively Associated with Mu Opioid Receptor Levels and Immune Activation and Are Attenuated by Nicotine Dependence(2019)4 cited
• → Evidence for the expression of peptides derived from three opioid precursors in NG 108CC15 hybrid cells(1987)1 cited
• → Interaction of i.v. dynorphin A(1–13) with kappa and mu agonists in a thermal antinociception assay in rhesus monkeys(1994)