Orphanin FQ has an inhibitory effect on the guinea pig ileum and the mouse vas deferens

Ge Zhang, Thomas F. Murray, David K. Grandy

    Research output: Contribution to journalArticlepeer-review

    38 Scopus citations

    Abstract

    The activity of the recently isolated endogenous opioid-like peptide orphanin FQ (OFQ) was measured in two classical bioassays of opioid action. OFQ potently and concentration-dependently suppressed the electrically stimulated contractions of the guinea pig ileum (GPI) and the mouse vas deferens (MVD)) with EC50 values of 1.82 ± 0.16 and 2.97 ± 0.01 mM, and E(max) values of 56 ± 3% and 96 ± 4%, respectively. This effect of OFQ, in both the GPI and MVD, was insensitive to the opioid receptor antagonist naloxone. OFQ competed with [3H]diprenorphine binding to μ-, δ or κ- opioid receptors stably expressed in Chinese hamster ovary cell lines with IC50 values of 2.1 ± 0.4, 2.2 ± 0.3, 0.75 ± 0.3 μM, respectively. Low affinity for the classical opioid receptors together with the inability of naloxone to antagonize its effect suggest that the inhibitory action of OFQ is mediated via a distinct OFQ receptor in the GPI and MVD. Consequently, the MVD could serve as a valuable bioassay of potential OFQ receptor antagonists.

    Original languageEnglish (US)
    Pages (from-to)102-106
    Number of pages5
    JournalBrain research
    Volume772
    Issue number1-2
    DOIs
    StatePublished - Oct 24 1997

    Keywords

    • Dynorphin A(1-13)NH
    • Guinea pig ileum
    • LC132 receptor
    • Mouse vas deferens
    • Naloxone
    • Nociceptin
    • Orphanin FQ
    • [D-Pen,D-Pen]]Enkephalin

    ASJC Scopus subject areas

    • Neuroscience(all)
    • Molecular Biology
    • Clinical Neurology
    • Developmental Biology

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