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

Research output: Contribution to journalArticlepeer-review

100 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 languageEnglish (US)
Pages (from-to)1713-1716
Number of pages4
JournalJournal of medicinal chemistry
Volume48
Issue number6
DOIs
StatePublished - Mar 24 2005

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