14-desoxy analogues of naltrindole and 7-spiroindanyloxymorphone: The role of the 14-hyroxy group at δ opioid receptors

Tushar A. Kshirsagar, Xinqin Fang, Philip S. Portoghese

Research output: Contribution to journalArticle

9 Scopus citations

Abstract

The 14-hydroxy group is known to increase the antagonist potency of μ- selective opioid ligands. To investigate the role of this group at the δ opioid receptor, the 14-desoxy analogues (7 and 9) of the δ-selective ligands, naltrindole (1, NT1) and spiroindanyloxymorphone (2, SIOM), have been synthesized and tested. The in vitro pharmacologic activities of 7 and 9 suggest that the 14-hydroxy group plays an important role in determining the δ selectivity and potency of NT1 and SIOM.

Original languageEnglish (US)
Pages (from-to)2657-2660
Number of pages4
JournalJournal of medicinal chemistry
Volume41
Issue number14
DOIs
StatePublished - Jul 2 1998

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