Stilbenes as κ-Selective, Non-nitrogenous Opioid Receptor Antagonists

[Image: see text] The natural stilbene pawhuskin A has been shown to function as an opioid receptor antagonist, with preferential binding to the κ receptor. This finding encouraged assembly of a set of analogues to probe the importance of key structural features. Assays on these compounds determined...

Descripción completa

Detalles Bibliográficos
Autores principales: Hartung, Alyssa M., Beutler, John A., Navarro, Hernán A., Wiemer, David F., Neighbors, Jeffrey D.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society and American Society of Pharmacognosy 2014
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3993902/
https://www.ncbi.nlm.nih.gov/pubmed/24456556
http://dx.doi.org/10.1021/np4009046
_version_ 1782312633947389952
author Hartung, Alyssa M.
Beutler, John A.
Navarro, Hernán A.
Wiemer, David F.
Neighbors, Jeffrey D.
author_facet Hartung, Alyssa M.
Beutler, John A.
Navarro, Hernán A.
Wiemer, David F.
Neighbors, Jeffrey D.
author_sort Hartung, Alyssa M.
collection PubMed
description [Image: see text] The natural stilbene pawhuskin A has been shown to function as an opioid receptor antagonist, with preferential binding to the κ receptor. This finding encouraged assembly of a set of analogues to probe the importance of key structural features. Assays on these compounds determined that one (compound 29) shows potent opioid receptor binding activity and significantly improved selectivity for the κ receptor. These studies begin to illuminate the structural features of these non-nitrogenous opioid receptor antagonists that are required for activity.
format Online
Article
Text
id pubmed-3993902
institution National Center for Biotechnology Information
language English
publishDate 2014
publisher American Chemical Society and American Society of Pharmacognosy
record_format MEDLINE/PubMed
spelling pubmed-39939022015-01-23 Stilbenes as κ-Selective, Non-nitrogenous Opioid Receptor Antagonists Hartung, Alyssa M. Beutler, John A. Navarro, Hernán A. Wiemer, David F. Neighbors, Jeffrey D. J Nat Prod [Image: see text] The natural stilbene pawhuskin A has been shown to function as an opioid receptor antagonist, with preferential binding to the κ receptor. This finding encouraged assembly of a set of analogues to probe the importance of key structural features. Assays on these compounds determined that one (compound 29) shows potent opioid receptor binding activity and significantly improved selectivity for the κ receptor. These studies begin to illuminate the structural features of these non-nitrogenous opioid receptor antagonists that are required for activity. American Chemical Society and American Society of Pharmacognosy 2014-01-23 2014-02-28 /pmc/articles/PMC3993902/ /pubmed/24456556 http://dx.doi.org/10.1021/np4009046 Text en Copyright © 2014 American Chemical Society and American Society of Pharmacognosy
spellingShingle Hartung, Alyssa M.
Beutler, John A.
Navarro, Hernán A.
Wiemer, David F.
Neighbors, Jeffrey D.
Stilbenes as κ-Selective, Non-nitrogenous Opioid Receptor Antagonists
title Stilbenes as κ-Selective, Non-nitrogenous Opioid Receptor Antagonists
title_full Stilbenes as κ-Selective, Non-nitrogenous Opioid Receptor Antagonists
title_fullStr Stilbenes as κ-Selective, Non-nitrogenous Opioid Receptor Antagonists
title_full_unstemmed Stilbenes as κ-Selective, Non-nitrogenous Opioid Receptor Antagonists
title_short Stilbenes as κ-Selective, Non-nitrogenous Opioid Receptor Antagonists
title_sort stilbenes as κ-selective, non-nitrogenous opioid receptor antagonists
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3993902/
https://www.ncbi.nlm.nih.gov/pubmed/24456556
http://dx.doi.org/10.1021/np4009046
work_keys_str_mv AT hartungalyssam stilbenesaskselectivenonnitrogenousopioidreceptorantagonists
AT beutlerjohna stilbenesaskselectivenonnitrogenousopioidreceptorantagonists
AT navarrohernana stilbenesaskselectivenonnitrogenousopioidreceptorantagonists
AT wiemerdavidf stilbenesaskselectivenonnitrogenousopioidreceptorantagonists
AT neighborsjeffreyd stilbenesaskselectivenonnitrogenousopioidreceptorantagonists

Ejemplares similares