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    Evaluation of edonerpic maleate as a CRMP2 inhibitor for pain relief

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    Author
    Moutal, Aubin
    Shan, Zhiming
    Miranda, Victor G
    François-Moutal, Liberty
    Madura, Cynthia L
    Khanna, May
    Khanna, Rajesh
    Affiliation
    Univ Arizona, Ctr Innovat Brain Sci
    Univ Arizona Hlth Sci, Coll Med, Dept Pharmacol
    Issue Date
    2019-11-02
    Keywords
    CRMP2
    DRG sensory neuron
    edonerpic maleate
    ion channels
    post-surgical pain
    
    Metadata
    Show full item record
    Publisher
    TAYLOR & FRANCIS INC
    Citation
    Aubin Moutal, Zhiming Shan, Victor G. Miranda, Liberty François-Moutal, Cynthia L. Madura, May Khanna & Rajesh Khanna (2019) Evaluation of edonerpic maleate as a CRMP2 inhibitor for pain relief, Channels, 13:1, 498-504, DOI: 10.1080/19336950.2019.1684608
    Journal
    CHANNELS
    Rights
    Copyright © 2019 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
    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
    We have previously reported that the microtubule-associated collapsin response mediator protein 2 (CRMP2) is necessary for the expression of chronic pain. CRMP2 achieves this control of nociceptive signaling by virtue of its ability to regulate voltage-gated calcium and sodium channels. To date, however, no drugs exist that target CRMP2. Recently, the small molecule edonerpic maleate (1 -{3-[2-(1-benzothiophen-5-yl)ethoxy]propyl}azetidin-3-ol maleate), a candidate therapeutic for Alzheimer’s disease was reported to be a novel CRMP2 binding compound with the potential to decrease its phosphorylation level in cortical tissues in vivo. Here we sought to determine the mechanism of action of edonerpic maleate and test its possible effect in a rodent model of chronic pain. We observed: (i) no binding between human CRMP2 and edonerpic maleate; (ii) edonerpic maleate had no effect on CRMP2 expression and phosphorylation in dorsal root ganglion (DRG) neurons; (iii) edonerpic maleate-decreased calcium but increased sodium current density in DRG neurons; and (iv) edonerpic maleate was ineffective in reversing post-surgical allodynia in male and female mice. Thus, while CRMP2 inhibiting compounds remain a viable strategy for developing new mechanism-based pain inhibitors, edonerpic maleate is an unlikely candidate.
    Note
    Open access journal
    ISSN
    1933-6950
    PubMed ID
    31680630
    DOI
    10.1080/19336950.2019.1684608
    Version
    Final published version
    Sponsors
    National Institutes of HealthUnited States Department of Health & Human ServicesNational Institutes of Health (NIH) - USA [1R01NS098772, 1R01DA042852, R01AT009716]
    ae974a485f413a2113503eed53cd6c53
    10.1080/19336950.2019.1684608
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