Binaltorphimine and nor-binaltorphimine, potent and selective k-opioid receptor antagonists

P. S. Portoghese; A. W. Lipkowski; A. E. Takemori

doi:10.1016/0024-3205(87)90585-6

Binaltorphimine and nor-binaltorphimine, potent and selective _k-opioid receptor antagonists

P. S. Portoghese, A. W. Lipkowski, A. E. Takemori

Research output: Contribution to journal › Article › peer-review

530 Scopus citations

Abstract

The opioid antagonist activities of two bivalent ligands, BNI and nor-BNI, have been evaluated in smooth muscle preparations and in mice. Both ligands are highly potent and selective as _k opioid receptor antagonists, with relatively feeble blocking activity at μ and δ opioid receptors. BNI and nor-BNI represent the first highly selective _k opioid receptor antagonists and should be of great utility as molecular probes for identifying the interaction of agonist ligands with _k opioid receptors in vitro and in vivo.

Original language	English (US)
Pages (from-to)	1287-1292
Number of pages	6
Journal	Life Sciences
Volume	40
Issue number	13
DOIs	https://doi.org/10.1016/0024-3205(87)90585-6
State	Published - Mar 30 1987
Externally published	Yes

Bibliographical note

Funding Information:
This investigation was supported by the National Institute on Drug Abuse. We thank Michael Powers, Barbara Taylor and Mary ~chwartz for their competent technical assistance.

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10.1016/0024-3205(87)90585-6

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abstract = "The opioid antagonist activities of two bivalent ligands, BNI and nor-BNI, have been evaluated in smooth muscle preparations and in mice. Both ligands are highly potent and selective as k opioid receptor antagonists, with relatively feeble blocking activity at μ and δ opioid receptors. BNI and nor-BNI represent the first highly selective k opioid receptor antagonists and should be of great utility as molecular probes for identifying the interaction of agonist ligands with k opioid receptors in vitro and in vivo.",

author = "Portoghese, \{P. S.\} and Lipkowski, \{A. W.\} and Takemori, \{A. E.\}",

note = "Funding Information: This investigation was supported by the National Institute on Drug Abuse. We thank Michael Powers, Barbara Taylor and Mary \textasciitilde{}chwartz for their competent technical assistance.",

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AU - Portoghese, P. S.

AU - Lipkowski, A. W.

AU - Takemori, A. E.

N1 - Funding Information: This investigation was supported by the National Institute on Drug Abuse. We thank Michael Powers, Barbara Taylor and Mary ~chwartz for their competent technical assistance.

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Y1 - 1987/3/30

N2 - The opioid antagonist activities of two bivalent ligands, BNI and nor-BNI, have been evaluated in smooth muscle preparations and in mice. Both ligands are highly potent and selective as k opioid receptor antagonists, with relatively feeble blocking activity at μ and δ opioid receptors. BNI and nor-BNI represent the first highly selective k opioid receptor antagonists and should be of great utility as molecular probes for identifying the interaction of agonist ligands with k opioid receptors in vitro and in vivo.

AB - The opioid antagonist activities of two bivalent ligands, BNI and nor-BNI, have been evaluated in smooth muscle preparations and in mice. Both ligands are highly potent and selective as k opioid receptor antagonists, with relatively feeble blocking activity at μ and δ opioid receptors. BNI and nor-BNI represent the first highly selective k opioid receptor antagonists and should be of great utility as molecular probes for identifying the interaction of agonist ligands with k opioid receptors in vitro and in vivo.

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