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Delta opioid receptor mediates phospholipase C activation via Gi in Xenopus oocytes

T Miyamae1, N Fukushima, Y Misu

  • 1Department of Pharmacology, Yokohama City University School of Medicine, Japan.

FEBS Letters
|November 1, 1993
PubMed

Insights

The opioid delta receptor (DOR1) activates phospholipase C via Gi1 protein, triggering a calcium-dependent chloride current in Xenopus oocytes. This signaling pathway is specific to delta-opioid agonists and Gi1 coupling.

Area of Science:

  • Neuropharmacology
  • Molecular Biology
  • Cell Signaling

Background:

  • The delta-subtype opioid receptor (DOR1) plays a role in various physiological processes.
  • Understanding the signal transduction pathways of opioid receptors is crucial for drug development.

Purpose of the Study:

  • To investigate the signal transduction mechanism of the cloned mouse delta-subtype opioid receptor (DOR1).
  • To determine the specific G protein coupling involved in DOR1 activation.

Main Methods:

  • Expression of DOR1 mRNA and G protein alpha subunits (Gi1, Gq, G(o)) in Xenopus oocytes.
  • Measurement of opioid delta-agonist-induced currents using electrophysiology.
  • Assessment of antagonist effects using naltrindol.

Main Results:

  • Delta-opioid agonists evoked a calcium-dependent chloride current in oocytes expressing DOR1 and Gi1 alpha subunit.
  • This agonist-induced current was blocked by the delta-specific antagonist naltrindol.
  • Minimal or no current was observed when oocytes expressed Gq or G(o) alpha subunits, indicating Gi1 specificity.

Conclusions:

  • The opioid delta-receptor functionally couples to phospholipase C through the activation of the Gi1 protein.
  • This study elucidates a specific signaling pathway for DOR1 activation, highlighting its interaction with Gi1.

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