Morphine promotes phosphorylation of the human delta-opioid receptor at serine 363

Eur J Pharmacol. 2005 Sep 20;519(3):212-4. doi: 10.1016/j.ejphar.2005.07.024.

Abstract

After prolonged stimulation, the delta-opioid receptor becomes desensitized by regulatory mechanisms such as receptor phosphorylation, internalization and down-regulation. In this study, we demonstrate that morphine treatment causes phosphorylation of S363 in the C-terminus of the human delta-opioid receptor. Morphine-mediated phosphorylation reached 53+/-8% of maximum deltorphin II-mediated phosphorylation. Phosphorylation of S363 may contribute to delta-opioid receptor desensitization by morphine.

Publication types

  • Comparative Study
  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Amino Acid Substitution
  • Animals
  • CHO Cells
  • Cricetinae
  • Cricetulus
  • Humans
  • Morphine / pharmacology*
  • Mutation
  • Oligopeptides / pharmacology
  • Phosphorylation / drug effects
  • Receptors, Opioid, delta / agonists
  • Receptors, Opioid, delta / genetics
  • Receptors, Opioid, delta / metabolism*
  • Serine / genetics
  • Serine / metabolism

Substances

  • Oligopeptides
  • Receptors, Opioid, delta
  • deltorphin II, Ala(2)-
  • Serine
  • Morphine