Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2007 May 3;50(9):2254-8.
doi: 10.1021/jm061327z. Epub 2007 Apr 4.

Pharmacological properties of bivalent ligands containing butorphan linked to nalbuphine, naltrexone, and naloxone at mu, delta, and kappa opioid receptors

Xuemei Peng  1 , Brian I Knapp, Jean M Bidlack, John L Neumeyer
Affiliations

Pharmacological properties of bivalent ligands containing butorphan linked to nalbuphine, naltrexone, and naloxone at mu, delta, and kappa opioid receptors

Xuemei Peng et al. J Med Chem. .

Abstract

Our investigation of bivalent ligands at mu, delta, and kappa opioid receptors is focused on the preparation of ligands containing kappa agonist and mu agonist/antagonist pharmacophores at one end joined by a chain containing the mu antagonist pharmacophores (naltrexone, naloxone, or nalbuphine) at the other end. These ligands were evaluated in vitro by their binding affinity at mu, delta, and kappa opioid receptors and their relative efficacy in the [35S]GTPgammaS assay.

PubMed Disclaimer

Figures

Fig. 1
Fig. 1
Structures of opioids and bivalent ligands
See this image and copyright information in PMC

Similar articles

See all similar articles

Cited by

See all "Cited by" articles

References

    1. Brady LS, Devi LA. Dimerization of G-protein-coupled receptors: Implications for drug design and signaling. Neuropsychopharmacol. 2000;23:S1–S77. - PubMed
    1. Devi LA. Heterodimerization of G-protein-coupled receptors: pharmacology, signaling and trafficking. Trends Pharmacol. Sci. 2001;22:532–537. - PubMed
    1. Gomes I, Jordan BA, Gupta A, Rois C, Trapaidze N, Devi LA. G-Protein coupled receptor dimerization : implications in modulating receptor function. J. Mol. Chem. 2001;79:226–242. - PubMed
    1. Morphy R, Kay C, Rankovic Z. From magic bullets to designed multiple ligands. Drug Discovery Today. 2004;9:641–651. - PubMed
    1. Cvejic S, Devi L. Dimerization of the δ Opioid Receptor: Implication for a role in receptor internalization. J. Biol. Chem. 1997;272:26959–26964. - PubMed
    2. Jordan BA, Cvejic S, Devi LA. Opioids and their complicated receptor complexes. Neuropsychopharm. 2000;23:S15–S18. - PubMed
    3. George SR, Fan T, Xie Z, Tse R, Tamni V, Varghese G, O’Dowd BF. Oligomerization of μ- and δ-opioid receptors: generation of novel functional properties. J. Biol. Chem. 2000;275:26128–26135. - PubMed

Publication types

MeSH terms