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

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

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    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 1 1995

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    ASJC Scopus subject areas

    • Molecular Medicine
    • Pharmacology

    Cite this

    Henry, D. J., Grandy, D. K., 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.