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

Ge Zhang, Thomas F. Murray, David Grandy

    Research output: Contribution to journalArticle

    38 Citations (Scopus)

    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

    Fingerprint

    Vas Deferens
    Ileum
    Guinea Pigs
    Opioid Receptors
    Naloxone
    Biological Assay
    Diprenorphine
    Opioid Peptides
    Narcotic Antagonists
    Cricetulus
    Opioid Analgesics
    Inhibitory Concentration 50
    Ovary
    nociceptin
    Cell Line

    Keywords

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

    ASJC Scopus subject areas

    • Neuroscience(all)

    Cite this

    Orphanin FQ has an inhibitory effect on the guinea pig ileum and the mouse vas deferens. / Zhang, Ge; Murray, Thomas F.; Grandy, David.

    In: Brain Research, Vol. 772, No. 1-2, 24.10.1997, p. 102-106.

    Research output: Contribution to journalArticle

    Zhang, Ge ; Murray, Thomas F. ; Grandy, David. / Orphanin FQ has an inhibitory effect on the guinea pig ileum and the mouse vas deferens. In: Brain Research. 1997 ; Vol. 772, No. 1-2. pp. 102-106.
    @article{8bbc8c5f4c2949408c16155bda526072,
    title = "Orphanin FQ has an inhibitory effect on the guinea pig ileum and the mouse vas deferens",
    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.",
    keywords = "[D-Pen,D-Pen]]Enkephalin, Dynorphin A(1-13)NH, Guinea pig ileum, LC132 receptor, Mouse vas deferens, Naloxone, Nociceptin, Orphanin FQ",
    author = "Ge Zhang and Murray, {Thomas F.} and David Grandy",
    year = "1997",
    month = "10",
    day = "24",
    doi = "10.1016/S0006-8993(97)00858-5",
    language = "English (US)",
    volume = "772",
    pages = "102--106",
    journal = "Brain Research",
    issn = "0006-8993",
    publisher = "Elsevier",
    number = "1-2",

    }

    TY - JOUR

    T1 - Orphanin FQ has an inhibitory effect on the guinea pig ileum and the mouse vas deferens

    AU - Zhang, Ge

    AU - Murray, Thomas F.

    AU - Grandy, David

    PY - 1997/10/24

    Y1 - 1997/10/24

    N2 - 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.

    AB - 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.

    KW - [D-Pen,D-Pen]]Enkephalin

    KW - Dynorphin A(1-13)NH

    KW - Guinea pig ileum

    KW - LC132 receptor

    KW - Mouse vas deferens

    KW - Naloxone

    KW - Nociceptin

    KW - Orphanin FQ

    UR - http://www.scopus.com/inward/record.url?scp=0030728717&partnerID=8YFLogxK

    UR - http://www.scopus.com/inward/citedby.url?scp=0030728717&partnerID=8YFLogxK

    U2 - 10.1016/S0006-8993(97)00858-5

    DO - 10.1016/S0006-8993(97)00858-5

    M3 - Article

    C2 - 9406961

    AN - SCOPUS:0030728717

    VL - 772

    SP - 102

    EP - 106

    JO - Brain Research

    JF - Brain Research

    SN - 0006-8993

    IS - 1-2

    ER -