Absence of nalbuphine anti-analgesia in the rat

Neurosci Lett. 2003 Jul 24;345(3):165-8. doi: 10.1016/s0304-3940(03)00538-x.

Abstract

In humans, kappa agonist-antagonist opioids such as nalbuphine have been proposed to produce both analgesia and anti-analgesia by acting at distinct receptors. The anti-analgesia appears to be greater in men, which may contribute to the greater nalbuphine analgesia observed in women. Kappa agonist-antagonists are also known to produce sexually dimorphic antinociception in nonhuman species but are generally more potent in males; anti-analgesia has not been reported in animals. The aim of the present study was to determine if nalbuphine anti-analgesia can be detected in the rat. Since nalbuphine anti-analgesia is more sensitive to naloxone antagonism than its analgesic effect, low doses of naloxone were combined with nalbuphine. Using the Randall-Selitto paw-withdrawal test, nalbuphine (0.5-10 mg/kg) induced dose-dependent antinociception in the rat. The antinociceptive effect of nalbuphine (0.5 or 1 mg/kg) was not enhanced by lower doses of naloxone but was antagonized by higher doses. These data do not support the hypothesis that the naloxone-sensitive anti-analgesic effect of nalbuphine observed in humans is present in the rat and could explain, at least in part, the opposite direction of the sex differences for kappa agonist-antagonist opioid analgesia observed in these two species.

Publication types

  • Comparative Study

MeSH terms

  • Analgesia / methods
  • Analgesics, Opioid / pharmacology*
  • Animals
  • Dose-Response Relationship, Drug
  • Drug Interactions
  • Male
  • Multivariate Analysis
  • Nalbuphine / pharmacology*
  • Naloxone / pharmacology
  • Narcotic Antagonists / pharmacology
  • Pain Measurement / drug effects
  • Rats
  • Rats, Sprague-Dawley
  • Reaction Time
  • Receptors, Opioid, kappa / agonists*

Substances

  • Analgesics, Opioid
  • Narcotic Antagonists
  • Receptors, Opioid, kappa
  • Naloxone
  • Nalbuphine