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

518 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.

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

Access

10.1016/0024-3205(87)90585-6

OpenUrl availability

Full text

Cite this

@article{ffcc147160404eef9292dc5d1c9334b1,

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

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 ~chwartz for their competent technical assistance.",

year = "1987",

month = mar,

day = "30",

doi = "10.1016/0024-3205(87)90585-6",

language = "English (US)",

volume = "40",

pages = "1287--1292",

journal = "Life Sciences",

issn = "0024-3205",

publisher = "Elsevier Inc.",

number = "13",

}

TY - JOUR

T1 - Binaltorphimine and nor-binaltorphimine, potent and selective k-opioid receptor antagonists

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.

PY - 1987/3/30

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.

UR - http://www.scopus.com/inward/record.url?scp=0023139286&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0023139286&partnerID=8YFLogxK

U2 - 10.1016/0024-3205(87)90585-6

DO - 10.1016/0024-3205(87)90585-6

M3 - Article

C2 - 2882399

AN - SCOPUS:0023139286

SN - 0024-3205

VL - 40

SP - 1287

EP - 1292

JO - Life Sciences

JF - Life Sciences

IS - 13

ER -