κ-Opioid receptors couple to inwardly rectifying potassium channels when coexpressed by Xenopus oocytes

Douglas J. Henry, David Grandy, Henry A. Lester, Norman Davidson, Charles Chavkin

    Research output: Contribution to journalArticle

    92 Citations (Scopus)

    Abstract

    Xenopus oocytes expressed κ-opioid specific binding sites after injection of cRNA prepared from a clone of the rat κ-opioid receptor. Coinjection of κ receptor cRNA with cRNA coding for a G protein-linked, inwardly rectifying, K+ channel (GIRK1, or KGA) resulted in oocytes that responded to the κ agonist U-69593 by activating a large (1.0-1.5-μA) K+ current. U- 69593 exhibited an EC50 of 260 ± 50 nM and was blocked by the opioid antagonists norbinaltorphimine and naloxone. The κ agonist bremazocine was 200-fold more potent than U-69593 in eliciting K+ current but exhibited a partial agonist profile in this expression system. The present results indicate that stimulation of inwardly rectifying K+ channels may be a potential effector mechanism for κ-opioid receptors.

    Original languageEnglish (US)
    Pages (from-to)551-557
    Number of pages7
    JournalMolecular Pharmacology
    Volume47
    Issue number3
    StatePublished - Mar 1995

    Fingerprint

    Inwardly Rectifying Potassium Channel
    Complementary RNA
    Opioid Receptors
    Xenopus
    Oocytes
    Narcotic Antagonists
    Naloxone
    GTP-Binding Proteins
    Opioid Analgesics
    Clone Cells
    Binding Sites
    Injections
    U 69593

    ASJC Scopus subject areas

    • Pharmacology

    Cite this

    Henry, D. J., Grandy, D., Lester, H. A., Davidson, N., & Chavkin, C. (1995). κ-Opioid receptors couple to inwardly rectifying potassium channels when coexpressed by Xenopus oocytes. Molecular Pharmacology, 47(3), 551-557.

    κ-Opioid receptors couple to inwardly rectifying potassium channels when coexpressed by Xenopus oocytes. / Henry, Douglas J.; Grandy, David; Lester, Henry A.; Davidson, Norman; Chavkin, Charles.

    In: Molecular Pharmacology, Vol. 47, No. 3, 03.1995, p. 551-557.

    Research output: Contribution to journalArticle

    Henry, DJ, Grandy, D, Lester, HA, Davidson, N & Chavkin, C 1995, 'κ-Opioid receptors couple to inwardly rectifying potassium channels when coexpressed by Xenopus oocytes', Molecular Pharmacology, vol. 47, no. 3, pp. 551-557.
    Henry, Douglas J. ; Grandy, David ; Lester, Henry A. ; Davidson, Norman ; Chavkin, Charles. / κ-Opioid receptors couple to inwardly rectifying potassium channels when coexpressed by Xenopus oocytes. In: Molecular Pharmacology. 1995 ; Vol. 47, No. 3. pp. 551-557.
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