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

121 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

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SDG 3 Good Health and Well-being

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10.1021/jm034234f

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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).",

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AU - Kulkarni, Amol

AU - Xie, Zhihua

AU - Bhushan, Rashmi G.

AU - Portoghese, Philip S.

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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).

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