A bivalent ligand (KDAN-18) containing δ-antagonist and κ-agonist pharmacophores bridges δ2 and κ1 opioid receptor phenotype

David J. Daniels; Amol Kulkarni; Zhihua Xie; Rashmi G. Bhushan; Philip S. Portoghese

doi:10.1021/jm034234f

A bivalent ligand (KDAN-18) containing δ-antagonist and κ-agonist pharmacophores bridges δ₂ and κ₁ opioid receptor phenotype

David J. Daniels, Amol Kulkarni, Zhihua Xie, Rashmi G. Bhushan, Philip S. Portoghese

Medicinal Chemistry

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

119 Scopus citations

Abstract

To characterize δ- and κ-opioid receptor phenotypes, bivalent ligands (KDAN series) containing δ-antagonist (naltrindole) and κ₁-agonist (ICI-199,441) pharmacophores were synthesized and evaluated by the intrathecal route using the mouse tail-flick assay and binding studies. The data have suggested that KDAN-18 (2) bridges phenotypic δ₂- and K₁-receptors. A conceptual model is presented to explain the organizational differences between the opioid receptors that give rise to the phenotypes (δ₁, δ₂, κ₁, κ₂).

Original language	English (US)
Pages (from-to)	1713-1716
Number of pages	4
Journal	Journal of medicinal chemistry
Volume	48
Issue number	6
DOIs	https://doi.org/10.1021/jm034234f
State	Published - Mar 24 2005

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

Publisher link

10.1021/jm034234f

Find It

Find It at U of M Libraries

Cite this

@article{66293b85b6ee4610b70c38a4dd729180,

title = "A bivalent ligand (KDAN-18) containing δ-antagonist and κ-agonist pharmacophores bridges δ2 and κ1 opioid receptor phenotype",

abstract = "To characterize δ- and κ-opioid receptor phenotypes, bivalent ligands (KDAN series) containing δ-antagonist (naltrindole) and κ1-agonist (ICI-199,441) pharmacophores were synthesized and evaluated by the intrathecal route using the mouse tail-flick assay and binding studies. The data have suggested that KDAN-18 (2) bridges phenotypic δ2- and K1-receptors. A conceptual model is presented to explain the organizational differences between the opioid receptors that give rise to the phenotypes (δ1, δ2, κ1, κ2).",

author = "Daniels, {David J.} and Amol Kulkarni and Zhihua Xie and Bhushan, {Rashmi G.} and Portoghese, {Philip S.}",

year = "2005",

month = mar,

day = "24",

doi = "10.1021/jm034234f",

language = "English (US)",

volume = "48",

pages = "1713--1716",

journal = "Journal of medicinal chemistry",

issn = "0022-2623",

publisher = "American Chemical Society",

number = "6",

}

TY - JOUR

T1 - A bivalent ligand (KDAN-18) containing δ-antagonist and κ-agonist pharmacophores bridges δ2 and κ1 opioid receptor phenotype

AU - Daniels, David J.

AU - Kulkarni, Amol

AU - Xie, Zhihua

AU - Bhushan, Rashmi G.

AU - Portoghese, Philip S.

PY - 2005/3/24

Y1 - 2005/3/24

N2 - To characterize δ- and κ-opioid receptor phenotypes, bivalent ligands (KDAN series) containing δ-antagonist (naltrindole) and κ1-agonist (ICI-199,441) pharmacophores were synthesized and evaluated by the intrathecal route using the mouse tail-flick assay and binding studies. The data have suggested that KDAN-18 (2) bridges phenotypic δ2- and K1-receptors. A conceptual model is presented to explain the organizational differences between the opioid receptors that give rise to the phenotypes (δ1, δ2, κ1, κ2).

AB - To characterize δ- and κ-opioid receptor phenotypes, bivalent ligands (KDAN series) containing δ-antagonist (naltrindole) and κ1-agonist (ICI-199,441) pharmacophores were synthesized and evaluated by the intrathecal route using the mouse tail-flick assay and binding studies. The data have suggested that KDAN-18 (2) bridges phenotypic δ2- and K1-receptors. A conceptual model is presented to explain the organizational differences between the opioid receptors that give rise to the phenotypes (δ1, δ2, κ1, κ2).

UR - http://www.scopus.com/inward/record.url?scp=15444364860&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=15444364860&partnerID=8YFLogxK

U2 - 10.1021/jm034234f

DO - 10.1021/jm034234f

M3 - Article

C2 - 15771416

AN - SCOPUS:15444364860

SN - 0022-2623

VL - 48

SP - 1713

EP - 1716

JO - Journal of medicinal chemistry

JF - Journal of medicinal chemistry

IS - 6

ER -