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

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

Research output: Contribution to journalArticlepeer-review

501 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 languageEnglish (US)
Pages (from-to)1287-1292
Number of pages6
JournalLife Sciences
Volume40
Issue number13
DOIs
StatePublished - Mar 30 1987
Externally publishedYes

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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