Involvement of spinal tyrosine kinase in inflammatory and N-methyl-D-aspartate-induced hyperalgesia in rats

Eur J Pharmacol. 2003 May 16;468(3):191-8. doi: 10.1016/s0014-2999(03)01718-7.

Abstract

Phosphorylation of a subunit of N-methyl-D-aspartate (NMDA) receptor by protein tyrosine kinase (PTK) Src or Trk is known to enhance its channel activity. We examined whether a spinally administered selective PTK inhibitor, lavendustin A, which has high affinity for Src and Trk tyrosine kinases, could influence the development and maintenance of inflammatory hyperalgesia or NMDA-induced hyperalgesia. Inflammation was induced by injection of a mixture of carrageenan and kaolin into the tail base of rats. In another group of rats, hyperalgesia was induced by intrathecal administration of NMDA. Intrathecal administration of lavendustin A (1.0 microg) or NMDA receptor antagonist, (+)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cycloheptane-5,10-iminemaleate, MK-801 (3.0 microg) before injection of a mixture of carrageenan and kaolin or after the development of inflammation inhibited carrageenan-kaolin-induced mechanical hyperalgesia. Intrathecal injection of 1.0 microg NMDA produced thermal and mechanical hyperalgesia. Co-administration of 1.0 microg lavendustin A with NMDA significantly reduced the duration of spontaneous pain behaviour and inhibited NMDA-induced hyperalgesia. Lavendustin A itself did not cause any sedation, motor impairment or analgesia. Our results suggest that inhibition of PTK could be therapeutically effective as an analgesic in some NMDA receptor-mediated hyperalgesic states.

Publication types

  • Evaluation Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Carrageenan / administration & dosage
  • Carrageenan / adverse effects
  • Dizocilpine Maleate / administration & dosage
  • Dizocilpine Maleate / pharmacology
  • Hot Temperature
  • Hyperalgesia / chemically induced*
  • Hyperalgesia / complications
  • Hyperalgesia / prevention & control
  • Inflammation / chemically induced*
  • Inflammation / complications
  • Inflammation / prevention & control
  • Injections, Spinal
  • Kaolin / administration & dosage
  • Kaolin / adverse effects
  • Male
  • N-Methylaspartate / administration & dosage*
  • N-Methylaspartate / adverse effects*
  • Pain
  • Pain Measurement
  • Phenols / administration & dosage
  • Phenols / pharmacokinetics
  • Protein-Tyrosine Kinases / administration & dosage*
  • Protein-Tyrosine Kinases / adverse effects*
  • Protein-Tyrosine Kinases / genetics
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, N-Methyl-D-Aspartate / drug effects
  • Spinal Cord / drug effects
  • Spinal Cord / enzymology*

Substances

  • Phenols
  • Receptors, N-Methyl-D-Aspartate
  • Kaolin
  • lavendustin A
  • N-Methylaspartate
  • Dizocilpine Maleate
  • Carrageenan
  • Protein-Tyrosine Kinases