Agonist and antagonist activities of ligands derived from naltrexone and oxymorphone

A. E. Takemori, M. Sultana, H. Nagase, P. S. Portoghese

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The pharmacological profile of naltrindole (NTI) and three of its analogues, N-methyl-NTI (N-Me-NTI), oxymorphindole (OMI) and naltriben (NTB) were studied in antinociceptive assays. The compounds were found to have agonist activities that appear to be mediated mainly by κ opioid receptors because norbinaltorphimine (nor-BNI), the selective κ opioid receptor antagonist inhibited their effects significantly. All of the compounds, behaved as antagonists at doses that were lower than those that produced agonist effects and they possessed a profilethat was very selective for inhibiting the antinociceptive activities of δ opioid receptor agonists. Differential antagonism by NTB of the activities of DSLET and DPDPE was demonstrated.

Original languageEnglish (US)
Pages (from-to)1491-1495
Number of pages5
JournalLife Sciences
Issue number20
StatePublished - 1992

Bibliographical note

Funding Information:
This investigation was supported by U. S. Public Service Grants from the National Institute on Drug Abuse. We thank the technical assistance of Mary Lunzer.

Copyright 2014 Elsevier B.V., All rights reserved.


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