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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82 Scopus citations


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

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