2. Academic Validation
  3. 14-O-Heterocyclic-substituted naltrexone derivatives as non-peptide mu opioid receptor selective antagonists: design, synthesis, and biological studies

14-O-Heterocyclic-substituted naltrexone derivatives as non-peptide mu opioid receptor selective antagonists: design, synthesis, and biological studies

  • Bioorg Med Chem Lett. 2009 Mar 15;19(6):1825-9. doi: 10.1016/j.bmcl.2008.12.093.
Guo Li 1,  Lindsey C K Aschenbach,  Hengjun He,  Dana E Selley,  Yan Zhang
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Virginia Commonwealth University, 410 North 12th Street, PO Box 980613, Richmond, VA 23298-0613, USA.
PMID: 19217280 DOI: 10.1016/j.bmcl.2008.12.093
Abstract

Mu Opioid Receptor antagonists have clinical utility and are important research tools. To develop non-peptide and highly selective mu Opioid Receptor Antagonist, a series of 14-O-heterocyclic-substituted naltrexone derivatives were designed, synthesized, and evaluated. These compounds showed subnanomolar-to-nanomolar binding affinity for the mu Opioid Receptor. Among them, compound 1 exhibited the highest selectivity for the mu Opioid Receptor over the delta and kappa receptors. These results implicated an alternative 'address' domain in the extracellular loops of the mu Opioid Receptor.

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