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Sci. STKE, 11 January 2000
Vol. 2000, Issue 14, p. tw7
[DOI: 10.1126/stke.2000.14.tw7]

EDITORS' CHOICE

OPIOID RECEPTORS Feeling Less Pain

Abstract: 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 ß-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 ß-arrestin 2. There are actually four related arrestins, but animals lacking just ß-arrestin 2 showed increased and prolonged pain-relieving effects of morphine. Thus, ß-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 ß-arrestin 2. Science 286: 2495-2498. [Abstract] [Full Text]

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

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Science Signaling. ISSN 1937-9145 (pre-2008: Science's STKE. ISSN 1525-8882)