• Neuroscience · Nov 1996

    Orphanin FQ is a functional anti-opioid peptide.

    • J S Mogil, J E Grisel, R K Reinscheid, O Civelli, J K Belknap, and D K Grandy.
    • Research Service, VA Medical Center, Portland, OR 97201, USA.
    • Neuroscience. 1996 Nov 1; 75 (2): 333337333-7.

    AbstractThe heptadecapeptide orphanin FQ has recently been shown to be the endogenous agonist for the orphan opioid-like receptor, LC132. The molecular evidence that LC132 and orphanin FQ are evolutionarily related to other opioid receptors and their ligands suggests that these proteins may also play a role in modulating opiate actions. We now report that orphanin FQ (0.5-10 nmol), injected intracerebroventricularly in mice, does not produce hyperalgesia as suggested previously but rather reverses opioid-mediated (i.e. naloxone-sensitive) stress-induced antinociception in three different algesiometric assays. In addition to its antagonism of endogenous opioid antinociception, orphanin FQ dose-dependently (2.5-25 nmol) reverses systemic morphine antinociception (5 mg/kg, s.c.). Based on these data, we propose that orphanin FQ is a functional anti-opioid peptide.

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