A bivalent ligand (KMN-21) antagonist for μ/κ heterodimeric opioid receptors

Shijun Zhang, Ajay Yekkirala, Ye Tang, Philip S Portoghese

Research output: Contribution to journalArticle

27 Citations (Scopus)

Abstract

In an effort to develop antagonists for κ-μ opioid receptor heterodimers, a series of bivalent ligands 3-6 containing κ- and μ-antagonist pharmacophores were designed and synthesized. Evaluation of the series in HEK-293 cells revealed 4 (KMN-21) to selectively antagonize the activation of κ-μ heterodimers, suggesting possible bridging of receptors when the bivalent ligand spacer contains 21 atoms.

Original languageEnglish (US)
Pages (from-to)6978-6980
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Volume19
Issue number24
DOIs
StatePublished - Dec 15 2009

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Narcotic Antagonists
Ligands
HEK293 Cells
Chemical activation
Atoms

Keywords

  • Bivalent ligand
  • Dimerization
  • Heterodimers
  • Opioid receptors

Cite this

A bivalent ligand (KMN-21) antagonist for μ/κ heterodimeric opioid receptors. / Zhang, Shijun; Yekkirala, Ajay; Tang, Ye; Portoghese, Philip S.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 19, No. 24, 15.12.2009, p. 6978-6980.

Research output: Contribution to journalArticle

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