A bivalent ligand (KDN-21) reveals spinal δ and κ opioid receptors are organized as heterodimers that give rise to δ1 and δ2 phenotypes. Selective targeting of δ-κ heterodimers

Rashmi G. Bhushan, Shiv K. Sharma, Zhihua Xie, David J. Daniels, Philip S. Portoghese

Research output: Contribution to journalArticle

118 Scopus citations

Abstract

In view of recent pharmacological studies suggesting the existence of δ-κ opioid receptor heterodimers/oligomers in the spinal cord, we have synthesized and evaluated (intrathecally in mice) a series of bivalent ligands (KDN series) containing κ and δ antagonist pharmacophores. Pharmacological and binding data have provided evidence for the bridging of spinal δ-κ receptor heterodimers by KDN-21 and for their identification as δ1 and κ2. The selectivity profile of KDN-21 and the apparent absence of coupled δ 12 phenotypes in the brain suggest a new approach for targeting receptors.

Original languageEnglish (US)
Pages (from-to)2969-2972
Number of pages4
JournalJournal of Medicinal Chemistry
Volume47
Issue number12
DOIs
StatePublished - Jun 3 2004

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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