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Antagonist effects of beta-funaltrexamine and naloxonazine on alfentanil-induced antinociception and muscle rigidity in the rat

Academic Article
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Overview

authors

  • Negus, S. S.
  • Pasternak, G. W.
  • Koob, George
  • Weinger, M. B.

publication date

  • February 1993

journal

  • Journal of Pharmacology and Experimental Therapeutics  Journal

abstract

  • Alfentanil is a potent and short-acting mu opioid agonist that produces both antinociceptive effects and muscle rigidity. In the present study, the susceptibility of alfentanil-induced antinociception and rigidity to antagonism by the selective mu antagonist beta-funaltrexamine and the selective mu-1 antagonist naloxonazine was examined. Alfentanil (37.7-150.0 micrograms/kg) produced a dose-dependent increase both in antinociception as measured by the warm-water tail-dip assay and in rigidity as measured by electromyographic recording of the gastrocnemius muscle. Both beta-funaltrexamine (10.0 and 20.0 mg/kg) and naloxonazine (7.5 and 15.0 mg/kg) produced dose-dependent and parallel rightward shifts in the alfentanil dose-effect curves for both antinociception and rigidity. Furthermore, the alfentanil dose-effect curves for antinociception and rigidity were shifted to the right to a similar degree by any given pretreatment. These results suggest that alfentanil-induced antinociception in the warm-water tail-dip test and rigidity are mediated by pharmacologically similar populations of opioid receptors. More specifically, these results suggest that mu-1 opioid receptors mediate both alfentanil-induced antinociception and rigidity.

subject areas

  • Alfentanil
  • Analgesia
  • Animals
  • Electromyography
  • Male
  • Muscle Rigidity
  • Naloxone
  • Naltrexone
  • Narcotic Antagonists
  • Rats
  • Rats, Wistar
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Identity

International Standard Serial Number (ISSN)

  • 0022-3565

PubMed ID

  • 8437122
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Additional Document Info

start page

  • 739

end page

  • 745

volume

  • 264

issue

  • 2

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