Pharmacological characterization in vivo of the novel opiate, β-funaltrexamine

S. J. Ward, P. S. Portoghese, A. E. Takemori

Research output: Contribution to journalArticlepeer-review

279 Scopus citations

Abstract

The profile of action of β-funaltrexamine (β-FNA), the fumaramate methyl ester derivative of naltrexone, on antinociceptive tests in vivo was investigated. β-FNA demonstrated antinociceptive actions that were of short duration and that appeared to be mediated by kappa receptor interaction. In contrast, the antagonist actions of β-FNA were of remarkably long duration and were selective toward mu agonist interactions. This profile of action is consistent with the profile of action of β-FNA in vitro. The selective long-lasting antagonism of mu-mediated effects by β-FNA may be of great value in the elucidation of multiple opioid receptor function.

Original languageEnglish (US)
Pages (from-to)494-498
Number of pages5
JournalJournal of Pharmacology and Experimental Therapeutics
Volume220
Issue number3
StatePublished - 1982

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