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

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

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37 Scopus citations


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
Issue number24
StatePublished - Dec 15 2009

Bibliographical note

Funding Information:
We thank Mike Powers for capable technical assistance. This research is supported by grant DA01533 from National Institute on Drug Abuse .


  • Bivalent ligand
  • Dimerization
  • Heterodimers
  • Opioid receptors


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