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

Neurosurgery

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101 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

ASJC Scopus subject areas

Molecular Medicine
Drug Discovery

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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 - Bhushan, Rashmi G.

AU - Portoghese, Philip S.

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

Abstract

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