• J Pain · Feb 2019

    Pharmacological modulation of endogenous opioid activity to attenuate neuropathic pain in rats.

    • Nai-Jiang Liu, Emiliya M Storman, and Alan R Gintzler.
    • Department of Obstetrics and Gynecology, State University of New York, Downstate Medical Center, Brooklyn, New York.
    • J Pain. 2019 Feb 1; 20 (2): 235-243.

    AbstractWe showed previously that spinal metabotropic glutamate receptor 1 (mGluR1) signaling suppresses or facilitates (depending on the stage of estrous cycle) analgesic responsiveness to intrathecal endomorphin 2, a highly mu-opioid receptor-selective endogenous opioid. Spinal endomorphin 2 antinociception is suppressed during diestrus by mGluR1 when it is activated by membrane estrogen receptor alpha (mERα) and is facilitated during proestrus when mGluR1 is activated by glutamate. In the current study, we tested the hypothesis that in female rats subjected to spinal nerve ligation (SNL), the inhibition of spinal estrogen synthesis or blockade of spinal mERα/mGluR1 would be antiallodynic during diestrus, whereas during proestrus, mGluR1 blockade would worsen the mechanical allodynia. As postulated, following SNL, aromatase inhibition or mERα/mGluR1 blockade during diestrus markedly lessened the mechanical allodynia. This was observed only on the paw ipsilateral to SNL and was eliminated by naloxone, implicating endogenous opioid mediation. In contrast, during proestrus, mGluR1 blockade worsened the SNL-induced mechanical allodynia of the ipsilateral paw. Findings suggest menstrual cycle stage-specific drug targets for and the putative clinical utility of harnessing endogenous opioids for chronic pain management in women, as well as the value of, if not the necessity for, considering menstrual cycle stage in clinical trials thereof. PERSPECTIVE: Intrathecal treatments that enhance spinal endomorphin 2 analgesic responsiveness under basal conditions lessen mechanical allodynia in a chronic pain model. Findings provide a foundation for developing drugs that harness endogenous opioid antinociception for chronic pain relief, lessening the need for exogenous opioids and thus prescription opioid abuse.Copyright © 2018 the American Pain Society. Published by Elsevier Inc. All rights reserved.

      Pubmed     Full text   Copy Citation     Plaintext  

      Add institutional full text...

    Notes

     
    Knowledge, pearl, summary or comment to share?
    300 characters remaining
    help        
    You can also include formatting, links, images and footnotes in your notes
    • Simple formatting can be added to notes, such as *italics*, _underline_ or **bold**.
    • Superscript can be denoted by <sup>text</sup> and subscript <sub>text</sub>.
    • Numbered or bulleted lists can be created using either numbered lines 1. 2. 3., hyphens - or asterisks *.
    • Links can be included with: [my link to pubmed](http://pubmed.com)
    • Images can be included with: ![alt text](https://bestmedicaljournal.com/study_graph.jpg "Image Title Text")
    • For footnotes use [^1](This is a footnote.) inline.
    • Or use an inline reference [^1] to refer to a longer footnote elseweher in the document [^1]: This is a long footnote..

    hide…

What will the 'Medical Journal of You' look like?

Start your free 21 day trial now.

We guarantee your privacy. Your email address will not be shared.