Elsevier

Life Sciences

Volume 40, Issue 13, 30 March 1987, Pages 1287-1292
Life Sciences

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

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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.

References (16)

  • G.A. Olson et al.

    Peptides

    (1984)
  • R. Cotton et al.

    Eur. J. Pharmacol.

    (1984)
  • S.J. Ward et al.

    Eur. J. Pharmacol.

    (1982)
  • G. Hayashi et al.

    Eur. J. Pharmacol.

    (1971)
  • A.W. Lipkowski et al.

    Tetrahedron Lett.

    (1986)
  • P.S. Portoghese et al.

    Life Sci.

    (1985)
  • W.R. Martin

    Pharmacol. Rev.

    (1983)
  • H.S. Akil et al.

    Ann. Rev. Neurosci.

    (1984)
There are more references available in the full text version of this article.

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