Abstract
In an effort to develop antagonists for kappa-mu opioid receptor heterodimers, a series of bivalent ligands 3-6 containing kappa- and mu-antagonist pharmacophores were designed and synthesized. Evaluation of the series in HEK-293 cells revealed 4 (KMN-21) to selectively antagonize the activation of kappa-mu heterodimers, suggesting possible bridging of receptors when the bivalent ligand spacer contains 21 atoms.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Cell Line
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Guanidines / chemical synthesis
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Guanidines / chemistry*
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Guanidines / pharmacology
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Humans
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Ligands
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Naltrexone / analogs & derivatives*
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Naltrexone / chemical synthesis
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Naltrexone / chemistry
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Naltrexone / pharmacology
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Receptors, Opioid, kappa / antagonists & inhibitors*
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Receptors, Opioid, mu / antagonists & inhibitors*
Substances
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Guanidines
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KMN-21 compound
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Ligands
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Receptors, Opioid, kappa
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Receptors, Opioid, mu
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Naltrexone