trans-3,4-Dimethyl-4-(3-carboxamidophenyl)piperidines: A novel class of μ-Selective opioid antagonists

Bertrand Le Bourdonnec, Serge Belanger, Joel A. Cassel, Gabriel J. Stabley, Robert N. DeHaven, Roland E. Dolle

Research output: Contribution to journalArticlepeer-review

21 Scopus citations


trans-3,4-Dimethyl-4-(3-carboxamidophenyl)piperidines constitute a novel class of μ opioid receptor antagonists. The CONH2 group was found to be an effective isostere of the phenolic OH moiety. Structure-activity relationships at the piperidine nitrogen position led to the identification of several ligands displaying high affinity toward the cloned human μ opioid receptors, good selectivity μ/δ, μ/κ, and potent in vitro antagonist activity.

Original languageEnglish
Pages (from-to)4459-4462
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Issue number24
StatePublished - Dec 15 2003


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