The NK2 receptor antagonist SR48968 inhibits thalamic responses evoked by thermal but not mechanical nociception

Eur J Pharmacol. 1993 Jun 11;237(1):143-6. doi: 10.1016/0014-2999(93)90104-p.

Abstract

Extracellular recordings were made in the thalamic posterior nuclear group of anesthetized rats to study the effects of SR48968, a non-peptide NK2 receptor antagonist, on the responses evoked by thermal or mechanical nociceptive cutaneous stimulation. SR48968 (0.125-0.5 mg/kg, i.v. route) inhibited the responses to thermal stimulation while being ineffective on mechanically evoked responses in doses up to 2 mg/kg i.v. This effect was stereoselective since SR48965, the (R) enantiomer of SR48968 with a 2000-fold lower affinity for NK2 receptors, did not modify thermally evoked responses at a dose of 1 mg/kg i.v. These results support the notion that NK2 receptors are involved in thermal nociception.

MeSH terms

  • Animals
  • Benzamides / pharmacology*
  • Hot Temperature
  • Male
  • Neurokinin A / antagonists & inhibitors*
  • Pain Measurement / drug effects*
  • Physical Stimulation
  • Piperidines / pharmacology*
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Neurotransmitter / antagonists & inhibitors*
  • Receptors, Tachykinin
  • Stereoisomerism
  • Thalamic Nuclei / drug effects*

Substances

  • Benzamides
  • Piperidines
  • Receptors, Neurotransmitter
  • Receptors, Tachykinin
  • SR 48968
  • Neurokinin A