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 language | English (US) |
|---|---|
| Pages (from-to) | 6978-6980 |
| Number of pages | 3 |
| Journal | Bioorganic and Medicinal Chemistry Letters |
| Volume | 19 |
| Issue number | 24 |
| DOIs | |
| State | Published - 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 .
UN SDGs
This output contributes to the following UN Sustainable Development Goals (SDGs)
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SDG 3 Good Health and Well-being
Keywords
- Bivalent ligand
- Dimerization
- Heterodimers
- Opioid receptors
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