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 language | English (US) |
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Pages (from-to) | 551-557 |
Number of pages | 7 |
Journal | Molecular pharmacology |
Volume | 47 |
Issue number | 3 |
State | Published - Mar 1995 |
ASJC Scopus subject areas
- Molecular Medicine
- Pharmacology