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Sci. STKE, 11 January 2000
Vol. 2000, Issue 14, p. tw7
[DOI: 10.1126/scisignal.142000tw7]

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Opioid Receptors Feeling Less Pain

Morphine is widely used clinically for the treatment of severe pain. Bohn et al. show that this analgesic effect of morphine is enhanced in mice that lack the protein β-arrestin 2. Morphine produces its effects by binding to the μ opioid receptor, a heterotrimeric guanine nucleotide binding protein (G protein)-coupled receptor. However, the receptor has a desensitization mechanism through which it becomes phosphorylated and then interacts with the signaling inhibitor β-arrestin 2. There are actually four related arrestins, but animals lacking just β-arrestin 2 showed increased and prolonged pain-relieving effects of morphine. Thus, β-arrestin 2 appears to show specificity for the μ opioid receptor and to be required for its normal physiological response.

Bohn, L.M., Lefkowitz, R.J., Gainetdinov, R.R., Peppel, K., Caron, M.G., and Lin, F-T. (1999) Enhanced morphine analgesia in mice lacking β-arrestin 2. Science 286: 2495-2498. [Abstract] [Full Text]

Citation: Feeling Less Pain. Sci. STKE 2000, tw7 (2000).

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