Evidence that behavioral phenotypes of morphine in β-arr2-/- mice are due to the unmasking of JNK signaling

Neuropsychopharmacology. 2012 Jul;37(8):1953-62. doi: 10.1038/npp.2012.42. Epub 2012 Apr 11.

Abstract

The altered behavioral effects of morphine, but not most other mu agonists, in mice lacking β-arrestin 2, suggest that this scaffolding protein regulates the signaling cascade of this commonly used analgesic. One of the cascades that could be regulated by β-arrestin 2 is cJun-N-terminal kinase (JNK), which binds with β-arrestin 2 and modulates the analgesic effects of morphine. Using neurons lacking β-arrestin 2 (β-arr2-/-) to examine this interaction, we found that β-arr2-/- neurons show altered intracellular distribution of JNK and cJun, and that morphine, but not fentanyl, increased the nuclear localization of the phosphorylated, therefore activated, form of cJun, a JNK target in dorsal root ganglia neurons. This suggests that deleting β-arrestin 2 affects the JNK cascade. We therefore examined whether some of the behavioral phenotypes of mice lacking β-arrestin 2 could be a result of altered JNK signaling. Indeed, two different JNK inhibitors reversed the enhanced analgesic effect of morphine, a known phenotype of β-arr2-/- mice, to +/+ levels. Both the reduced locomotor effect of morphine and the psychomotor sensitization to repeated morphine administration in β-arr2-/- mice were also returned to +/+ levels by inhibiting JNK. In contrast, the behavioral effects of fentanyl were neither genotype-dependent nor affected by JNK inhibition. Furthermore, a PKC inhibitor had a similar effect as inhibiting JNK in reducing the enhanced analgesic effect of morphine in β-arr2-/- mice to +/+ levels. In summary, removing β-arrestin 2 reveals mu receptor activation of the JNK cascade in a ligand-specific manner explaining several behavioral phenotypes of β-arr2-/- mice.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Arrestins / genetics*
  • Cells, Cultured
  • Female
  • Fentanyl / pharmacology
  • Ganglia, Spinal / drug effects
  • Ganglia, Spinal / metabolism
  • Ganglia, Spinal / physiology
  • JNK Mitogen-Activated Protein Kinases / antagonists & inhibitors
  • JNK Mitogen-Activated Protein Kinases / metabolism*
  • Male
  • Membrane Potentials / drug effects
  • Membrane Potentials / physiology
  • Mice
  • Mice, Inbred C57BL
  • Mice, Knockout
  • Morphine / antagonists & inhibitors
  • Morphine / pharmacology*
  • Motor Activity / drug effects*
  • Pain Measurement / drug effects*
  • Phosphorylation
  • Protein Kinase C / antagonists & inhibitors
  • Proto-Oncogene Proteins c-jun / metabolism
  • Signal Transduction / drug effects*
  • beta-Arrestin 2
  • beta-Arrestins

Substances

  • Arrb2 protein, mouse
  • Arrestins
  • Proto-Oncogene Proteins c-jun
  • beta-Arrestin 2
  • beta-Arrestins
  • Morphine
  • Protein Kinase C
  • JNK Mitogen-Activated Protein Kinases
  • Fentanyl