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Enhanced morphine analgesia in mice lacking beta-arrestin 2.

Publication ,  Journal Article
Bohn, LM; Lefkowitz, RJ; Gainetdinov, RR; Peppel, K; Caron, MG; Lin, FT
Published in: Science
December 24, 1999

The ability of morphine to alleviate pain is mediated through a heterotrimeric guanine nucleotide binding protein (G protein)-coupled heptahelical receptor (GPCR), the mu opioid receptor (muOR). The efficiency of GPCR signaling is tightly regulated and ultimately limited by the coordinated phosphorylation of the receptors by specific GPCR kinases and the subsequent interaction of the phosphorylated receptors with beta-arrestin 1 and beta-arrestin 2. Functional deletion of the beta-arrestin 2 gene in mice resulted in remarkable potentiation and prolongation of the analgesic effect of morphine, suggesting that muOR desensitization was impaired. These results provide evidence in vivo for the physiological importance of beta-arrestin 2 in regulating the function of a specific GPCR, the muOR. Moreover, they suggest that inhibition of beta-arrestin 2 function might lead to enhanced analgesic effectiveness of morphine and provide potential new avenues for the study and treatment of pain, narcotic tolerance, and dependence.

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Published In

Science

DOI

ISSN

0036-8075

Publication Date

December 24, 1999

Volume

286

Issue

5449

Start / End Page

2495 / 2498

Location

United States

Related Subject Headings

  • beta-Arrestins
  • beta-Arrestin 2
  • beta-Arrestin 1
  • Signal Transduction
  • Receptors, Opioid, mu
  • Phosphorylation
  • Pain Threshold
  • Pain Measurement
  • Narcotic Antagonists
  • Naloxone
 

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Bohn, L. M., Lefkowitz, R. J., Gainetdinov, R. R., Peppel, K., Caron, M. G., & Lin, F. T. (1999). Enhanced morphine analgesia in mice lacking beta-arrestin 2. Science, 286(5449), 2495–2498. https://doi.org/10.1126/science.286.5449.2495
Bohn, L. M., R. J. Lefkowitz, R. R. Gainetdinov, K. Peppel, M. G. Caron, and F. T. Lin. “Enhanced morphine analgesia in mice lacking beta-arrestin 2.Science 286, no. 5449 (December 24, 1999): 2495–98. https://doi.org/10.1126/science.286.5449.2495.
Bohn LM, Lefkowitz RJ, Gainetdinov RR, Peppel K, Caron MG, Lin FT. Enhanced morphine analgesia in mice lacking beta-arrestin 2. Science. 1999 Dec 24;286(5449):2495–8.
Bohn, L. M., et al. “Enhanced morphine analgesia in mice lacking beta-arrestin 2.Science, vol. 286, no. 5449, Dec. 1999, pp. 2495–98. Pubmed, doi:10.1126/science.286.5449.2495.
Bohn LM, Lefkowitz RJ, Gainetdinov RR, Peppel K, Caron MG, Lin FT. Enhanced morphine analgesia in mice lacking beta-arrestin 2. Science. 1999 Dec 24;286(5449):2495–2498.
Journal cover image

Published In

Science

DOI

ISSN

0036-8075

Publication Date

December 24, 1999

Volume

286

Issue

5449

Start / End Page

2495 / 2498

Location

United States

Related Subject Headings

  • beta-Arrestins
  • beta-Arrestin 2
  • beta-Arrestin 1
  • Signal Transduction
  • Receptors, Opioid, mu
  • Phosphorylation
  • Pain Threshold
  • Pain Measurement
  • Narcotic Antagonists
  • Naloxone