Dynorphin inhibits NEP activity in R1.1 mouse thymoma cells

Cell Biochem Funct. 2008 Dec;26(8):916-9. doi: 10.1002/cbf.1524.

Abstract

NEP/CALLA or CD10 is an endopeptidase (E.C. 3.4.24.11) that inactivates numerous neuropeptides, including dynorphin. Dynorphin is an endogenous opioid polypeptide that binds to kappa-opioid receptors with greatest affinity. R1.1 mouse thymoma cells highly express kappa-opioid receptors. In this study, on R1.1 cells, NEP activity was inhibited by kappa-opioid polypeptide dynorphin (10(-8)-10(-6) M) and by thiorphan (2 x 10(-4) M), a known inhibitor of NEP (30 min treatment). NEP inhibition by dynorphin was stronger than by thiorphan. A non-opioid opioid mechanism of action was mostly involved in this inhibition.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Line, Tumor
  • Dynorphins / administration & dosage
  • Dynorphins / pharmacology*
  • Mice
  • Naltrexone / analogs & derivatives
  • Naltrexone / pharmacology
  • Narcotic Antagonists / pharmacology
  • Neprilysin / biosynthesis
  • Neprilysin / metabolism*
  • Receptors, Opioid, kappa / antagonists & inhibitors
  • Receptors, Opioid, kappa / metabolism
  • Thiophenes / pharmacology
  • Thymoma
  • Thymus Neoplasms

Substances

  • Narcotic Antagonists
  • Receptors, Opioid, kappa
  • Thiophenes
  • thiophane
  • norbinaltorphimine
  • Naltrexone
  • Dynorphins
  • Neprilysin