The irreversible narcotic antagonistic and reversible agonistic properties of the fumaramate methyl ester derivative of naltrexone

A. E. Takemori, Dennis L. Larson, P. S. Portoghese

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220 Scopus citations

Abstract

The fumaramate methyl ester derivatives of naltrexone (β-FNA) and oxymorphone (β-FOA) were both found to be reversible agonists on the guinea pig ileal longitudinal muscle preparation. In addition, β-FNA possessed an irreversible antagonistic effect against morphine whereas β-FOA had no such capacity. Analysis by pA2 values revealed that β-FOa resembled pure agonists like morphine and enkephalin while β-FNA resembled the mixed agonist-antagonists like nalorphine and pentazocine. The antagonism by β-FNA was very selective in that it antagonized pure agonists but had little or no effect on the effects of either mixed agonists, ethylketocyclazocine or other non-opiate-type agonists like norepinephrine.

Original languageEnglish (US)
Pages (from-to)445-451
Number of pages7
JournalEuropean Journal of Pharmacology
Volume70
Issue number4
DOIs
StatePublished - Apr 9 1981

Keywords

  • Agonist
  • Antagonist
  • Fumaramate methyl ester derivative
  • Guinea pig ileum
  • Naltrexone
  • Narcotic
  • Opioid receptor
  • Oxymophone

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