Agonist/antagonist properties of nalbuphine, butorphanol and (-)-pentazocine in male vs. female rats

Pharmacology, Biochemistry, and Behavior
R M Craft, D M McNiel

Abstract

To determine whether sex differences in the effects of mixed-action opioids could be due to differential activity at mu or kappa receptors, agonist/antagonist properties of nalbuphine, butorphanol and (-)-pentazocine were compared in male vs. female rats using a diuresis test. In water-loaded rats (2-h test), nalbuphine and (-)-pentazocine dose-dependently increased urination similarly in both sexes, whereas butorphanol increased urination more in females than in males on a ml/kg basis. The diuretic effects of all three opioids were at least partially blocked by the kappa receptor-selective antagonist nor-binaltorphimine (nor-BNI, 5 mg/kg) in both sexes. Kappa receptor-mediated antagonism of diuresis induced by U69,593 (0.56 mg/kg) was only observed with butorphanol in males. In water-loaded rats (1-h test), nalbuphine did not suppress, and butorphanol and (-)-pentazocine significantly suppressed urination in males only; all three mixed-action opioids dose-dependently blocked the antidiuretic effect of the selective mu agonist fentanyl (0.056 mg/kg) in both sexes. The ability of nalbuphine and (-)-pentazocine to block fentanyl-induced antidiuresis was not affected by pretreatment with nor-BNI in either sex. In contrast, the abi...Continue Reading

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Citations

May 5, 2011·European Journal of Pharmacology·Matthew F PetersTodd A Brugel
Nov 26, 2014·Academic Emergency Medicine : Official Journal of the Society for Academic Emergency Medicine·Paul I MuseySamuel A McLean
Oct 19, 2010·Life Sciences·Khampaseuth Rasakham, Lee-Yuan Liu-Chen
Jun 22, 2010·Heart & Lung : the Journal of Critical Care·Cynthia Arslanian-Engoren, Milo Engoren

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