Effect of beta-funaltrexamine on opioid side-effects produced by morphine and U-50, 488H

J Pharm Pharmacol. 1985 Nov;37(11):841-3. doi: 10.1111/j.2042-7158.1985.tb04985.x.

Abstract

Pretreatment of rats with the irreversible mu-opioid receptor antagonist, beta-funaltrexamine (beta-FNA), 20-40 mg kg-1 s.c., produced a dose-related antagonism of the reduction in respiratory rate, gastrointestinal (GI) propulsion, rotarod reaction latencies and body temperature produced by morphine administration 24 h later, suggesting that these effects are mediated via mu-opioid receptors. The kappa-receptor agonist, U-50,488H, was without effect on respiratory rate at the doses tested, but produced hypothermia, sedation and low maximum inhibition of GI propulsion. These effects of U-50,488H were not blocked by beta-FNA suggesting that they are mediated via kappa-receptors.

MeSH terms

  • 3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer
  • Analgesics / toxicity*
  • Animals
  • Body Temperature / drug effects
  • Depression, Chemical
  • Dose-Response Relationship, Drug
  • Gastrointestinal Motility / drug effects
  • Hypnotics and Sedatives
  • Male
  • Morphine / antagonists & inhibitors
  • Morphine / toxicity*
  • Naltrexone / analogs & derivatives*
  • Naltrexone / pharmacology
  • Narcotic Antagonists / pharmacology*
  • Pyrrolidines / toxicity*
  • Rats
  • Rats, Inbred Strains
  • Respiration / drug effects

Substances

  • Analgesics
  • Hypnotics and Sedatives
  • Narcotic Antagonists
  • Pyrrolidines
  • Naltrexone
  • 3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer
  • beta-funaltrexamine
  • Morphine