Naloxone's Pentapeptide Binding Site on Filamin A Blocks Mu Opioid Receptor–Gs Coupling and CREB Activation of Acute Morphine
2009

Naloxone's Role in Opioid Receptor Signaling

Sample size: 4 publication Evidence: high

Author Information

Author(s): Wang Hoau-Yan, Burns Lindsay H.

Primary Institution: City University of New York Medical School

Hypothesis

Ultra-low-dose naloxone prevents the switch in mu opioid receptor coupling from Gi/o to Gs, thereby attenuating opioid tolerance and dependence.

Conclusion

The study found that ultra-low-dose naloxone effectively blocks the acute morphine-induced switch in mu opioid receptor signaling, which is linked to opioid tolerance and dependence.

Supporting Evidence

  • Ultra-low-dose naloxone prevents the switch in mu opioid receptor coupling induced by morphine.
  • The study demonstrated that acute morphine causes a transient switch in G protein coupling from Gi/o to Gs.
  • Co-treatment with naloxone or naltrexone completely blocked the morphine-induced Gs coupling.

Takeaway

When you take a lot of morphine, it changes how your brain's receptors work, but a tiny bit of naloxone can stop that change and help prevent problems.

Methodology

The study used organotypic striatal slice cultures from male Sprague Dawley rats to assess the effects of morphine and naloxone on mu opioid receptor signaling.

Participant Demographics

Male Sprague Dawley rats (200 to 250 g)

Statistical Information

P-Value

p<0.01

Statistical Significance

p<0.05

Digital Object Identifier (DOI)

10.1371/journal.pone.0004282

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