کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1374214 | 981914 | 2009 | 5 صفحه PDF | دانلود رایگان |
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.
A series of 14-O-heterocyclic-substituted naltrexone derivatives were designed, synthesized, and evaluated. Among them, compound 1 showed binding affinity at subnanomolar level and highest selectivity for the mu opioid receptor.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 6, 15 March 2009, Pages 1825–1829