Agonist and antagonist activities of ligands derived from naltrexone and oxymorphone

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

doi:10.1016/0024-3205(92)90138-F

Agonist and antagonist activities of ligands derived from naltrexone and oxymorphone

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

Medicinal Chemistry

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Abstract

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 language	English (US)
Pages (from-to)	1491-1495
Number of pages	5
Journal	Life Sciences
Volume	50
Issue number	20
DOIs	https://doi.org/10.1016/0024-3205(92)90138-F
State	Published - 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:
Copyright 2014 Elsevier B.V., All rights reserved.

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10.1016/0024-3205(92)90138-F

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title = "Agonist and antagonist activities of ligands derived from naltrexone and oxymorphone",

abstract = "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.",

author = "Takemori, {A. E.} and M. Sultana and H. Nagase and Portoghese, {P. S.}",

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

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T1 - Agonist and antagonist activities of ligands derived from naltrexone and oxymorphone

AU - Takemori, A. E.

AU - Sultana, M.

AU - Nagase, H.

AU - Portoghese, P. S.

N1 - 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: Copyright 2014 Elsevier B.V., All rights reserved.

PY - 1992

Y1 - 1992

N2 - 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.

AB - 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.

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Agonist and antagonist activities of ligands derived from naltrexone and oxymorphone

Abstract

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