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

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Li G,Aschenbach LC,He H,Selley DE,Zhang Y

doi

10.1016/j.bmcl.2008.12.093

subject

Has Abstract

pub_date

2009-03-15 00:00:00

pages

1825-9

issue

6

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(08)01613-2

journal_volume

19

pub_type

杂志文章

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