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Bioorg Med Chem. 2010 May 15;18(10):3535-42. doi: 10.1016/j.bmc.2010.03.068. Epub 2010 Mar 29.

Synthesis and opioid activity of novel 6-substituted-6-demethoxy-ethenomorphinans.

Author information

1
Department of Organic Chemistry, University of Debrecen, PO Box 20, H-4010, Debrecen, Hungary.

Abstract

A set of novel 6-substituted orvinols was synthesized and pharmacologically characterized in order to explore the effect of the polarity and steric effects of these new moieties on the opioid activity. It was revealed that longer 6-O-alkyl chains led to increased agonistic activities, while the lack of C6-etheral oxygen gave rise to an antagonistic profile at the opioid receptors in the mouse ileum.

PMID:
20413312
DOI:
10.1016/j.bmc.2010.03.068
[Indexed for MEDLINE]

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