Stilbenes as κ-selective, non-nitrogenous opioid receptor antagonists

Alyssa M. Hartung; John A. Beutler; Hernán A. Navarro; David F. Wiemer; Jeffrey D. Neighbors

doi:10.1021/np4009046

Stilbenes as κ-selective, non-nitrogenous opioid receptor antagonists

Alyssa M. Hartung, John A. Beutler, Hernán A. Navarro, David F. Wiemer, Jeffrey D. Neighbors

Research output: Contribution to journal › Article › peer-review

13 Scopus citations

Abstract

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.

Original language	English (US)
Pages (from-to)	311-319
Number of pages	9
Journal	Journal of Natural Products
Volume	77
Issue number	2
DOIs	https://doi.org/10.1021/np4009046
State	Published - Feb 28 2014

All Science Journal Classification (ASJC) codes

Analytical Chemistry
Molecular Medicine
Pharmacology
Pharmaceutical Science
Drug Discovery
Complementary and alternative medicine
Organic Chemistry

Access to Document

10.1021/np4009046

Cite this

@article{b87e5d031da8431daec2262c92edaa23,

title = "Stilbenes as κ-selective, non-nitrogenous opioid receptor antagonists",

abstract = "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.",

author = "Hartung, {Alyssa M.} and Beutler, {John A.} and Navarro, {Hern{\'a}n A.} and Wiemer, {David F.} and Neighbors, {Jeffrey D.}",

year = "2014",

month = feb,

day = "28",

doi = "10.1021/np4009046",

language = "English (US)",

volume = "77",

pages = "311--319",

journal = "Journal of Natural Products",

issn = "0163-3864",

publisher = "American Chemical Society",

number = "2",

}

TY - JOUR

T1 - Stilbenes as κ-selective, non-nitrogenous opioid receptor antagonists

AU - Hartung, Alyssa M.

AU - Beutler, John A.

AU - Navarro, Hernán A.

AU - Wiemer, David F.

AU - Neighbors, Jeffrey D.

PY - 2014/2/28

Y1 - 2014/2/28

N2 - 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.

AB - 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.

UR - http://www.scopus.com/inward/record.url?scp=84896849447&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=84896849447&partnerID=8YFLogxK

U2 - 10.1021/np4009046

DO - 10.1021/np4009046

M3 - Article

C2 - 24456556

AN - SCOPUS:84896849447

SN - 0163-3864

VL - 77

SP - 311

EP - 319

JO - Journal of Natural Products

JF - Journal of Natural Products

IS - 2

ER -

Stilbenes as κ-selective, non-nitrogenous opioid receptor antagonists

Abstract

All Science Journal Classification (ASJC) codes

Access to Document

Other files and links

Fingerprint

Cite this