Protein kinase C inhibitor BIM suspended TRPV1 effect on mu-opioid receptor

Brain Res Bull. 2013 Jan:90:114-7. doi: 10.1016/j.brainresbull.2012.10.008. Epub 2012 Nov 2.

Abstract

The purpose of the present study was to elucidate the role of protein kinase A and C in the mechanism of capsaicin inhibition on mu-opiate receptors. H89, a protein kinase A inhibitor and BIM (bisindolylmaleimide), a protein kinase C inhibitor were used for this purpose. BIM suspended the inhibition of capsaicin in endomorphin-1 competition binding. The addition of BIM alone had no effect itself on this reaction. H89 however, exerted a strong inhibitory effect on the endomorphin-1 binding. We can conclude that protein kinase C certainly plays a role in the inhibition of capsaicin. The role of protein kinase A in this reaction could not be established, owing to the blocking effect of H89 on the mu-opioid receptors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Analgesics, Opioid / pharmacology
  • Animals
  • Brain / ultrastructure
  • Capsaicin / pharmacology
  • Cell Membrane / drug effects*
  • Dose-Response Relationship, Drug
  • Drug Interactions
  • Enzyme Inhibitors / pharmacology*
  • Indoles / pharmacology*
  • Male
  • Maleimides / pharmacology*
  • Oligopeptides / pharmacology
  • Radioligand Assay
  • Rats
  • Rats, Wistar
  • Receptors, Opioid, mu / metabolism*
  • Sensory System Agents / pharmacology
  • TRPV Cation Channels / metabolism*

Substances

  • Analgesics, Opioid
  • Enzyme Inhibitors
  • Indoles
  • Maleimides
  • Oligopeptides
  • Receptors, Opioid, mu
  • Sensory System Agents
  • TRPV Cation Channels
  • endomorphin 1
  • bisindolylmaleimide
  • Capsaicin