RP-67580, a specific tachykinin NK1 receptor antagonist, relieves chronic hyperalgesia in diabetic rats

Eur J Pharmacol. 1993 Sep 14;241(2-3):267-70. doi: 10.1016/0014-2999(93)90213-2.

Abstract

The effect of a non-peptide NK1 receptor antagonist, RP-67580, and of its enantiomer, RP-68651, on nociceptive thresholds in normal and streptozocin-induced diabetic rats submitted to paw pressure is reported. RP-67580 (1, 3, 9 mg/kg s.c.) dose dependently reduced the diabetes-induced mechanical hyperalgesia observed 4 weeks after induction of diabetes. In normal rats, RP-67580 failed to increase nociceptive thresholds. RP-68651 was inactive in both diabetic and normal rats. These results suggest that (i) substance P is involved in the diabetes-induced chronic hyperalgesia, and (ii) NK1 receptor antagonists merit to be studied more extensively in relation with this pathological condition.

MeSH terms

  • Analgesics / pharmacology*
  • Analysis of Variance
  • Animals
  • Diabetic Neuropathies / drug therapy*
  • Diabetic Neuropathies / physiopathology
  • Hyperalgesia / drug therapy*
  • Hyperalgesia / physiopathology
  • Indoles / pharmacology*
  • Isoindoles
  • Male
  • Neurokinin-1 Receptor Antagonists*
  • Rats
  • Rats, Sprague-Dawley
  • Stereoisomerism
  • Substance P / antagonists & inhibitors*
  • Substance P / physiology

Substances

  • Analgesics
  • Indoles
  • Isoindoles
  • Neurokinin-1 Receptor Antagonists
  • 7,7-diphenyl-2-(1-imino-2-(2-methoxyphenyl)ethyl)perhydroisoindol-4-one
  • Substance P