Ontology highlight
ABSTRACT:
SUBMITTER: Li G
PROVIDER: S-EPMC2802822 | biostudies-literature | 2009 Mar
REPOSITORIES: biostudies-literature
Li Guo G Aschenbach Lindsey C K LC He Hengjun H Selley Dana E DE Zhang Yan Y
Bioorganic & medicinal chemistry letters 20081229 6
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 im ...[more]