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    On resin click-chemistry-mediated synthesis of novel enkephalin analogues with potent anti-nociceptive activity

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    s41598-019-42289-5.pdf
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    Final Published Version
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    Author
    Stefanucci, Azzurra
    Lei, Wei
    Pieretti, Stefano
    Novellino, Ettore
    Dimmito, Marilisa Pia
    Marzoli, Francesca
    Streicher, John M
    Mollica, Adriano
    Affiliation
    Univ Arizona, Coll Med, Dept Pharmacol
    Issue Date
    2019-04-08
    
    Metadata
    Show full item record
    Publisher
    NATURE PUBLISHING GROUP
    Citation
    Stefanucci, A., Lei, W., Pieretti, S., Novellino, E., Dimmito, M. P., Marzoli, F., ... & Mollica, A. (2019). On resin click-chemistry-mediated synthesis of novel enkephalin analogues with potent anti-nociceptive activity. Scientific reports, 9(1), 5771.
    Journal
    SCIENTIFIC REPORTS
    Rights
    © The Author(s) 2019. Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in a credit line to the material. If material is not included in the article’s Creative Commons license and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder.
    Collection Information
    This item from the UA Faculty Publications collection is made available by the University of Arizona with support from the University of Arizona Libraries. If you have questions, please contact us at repository@u.library.arizona.edu.
    Abstract
    Here, we report the chemical synthesis of two DPDPE analogues 7a (NOVA1) and 7b (NOVA2). This entailed the solid-phase synthesis of two enkephalin precursor chains followed by a CuI-catalyzed azide-alkyne cycloaddition, with the aim of improving in vivo analgesic efficacy versus DPDPE. NOVA2 showed good affinity and selectivity for the μ-opioid receptor (KI of 59.2 nM, EC50 of 12.9 nM, EMax of 87.3%), and long lasting anti-nociceptive effects in mice when compared to DPDPE.
    Note
    Open access journal
    ISSN
    2045-2322
    PubMed ID
    30962495
    DOI
    10.1038/s41598-019-42289-5
    Version
    Final published version
    Sponsors
    University of Arizona
    ae974a485f413a2113503eed53cd6c53
    10.1038/s41598-019-42289-5
    Scopus Count
    Collections
    UA Faculty Publications

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