Journal
NEUROSCIENCE LETTERS
Volume 443, Issue 3, Pages 209-212Publisher
ELSEVIER IRELAND LTD
DOI: 10.1016/j.neulet.2008.07.088
Keywords
sinomenine; opioid mu-receptor; transfected cell; radioligand binding; receptor phosphorylation; antinociception; mouse
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Funding
- National Science Council [NSC 96-2320-B-006-030-MY3]
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Sinomenine, one of the alkaloids extracted from roots or stems of Sinomenium acutum, is documented to show antinociceptive action but the action mechanism is still unclear. The present study was aimed to investigate the effect of sinomenine on opioid mu-receptor (OMR). In Chinese Hamster Ovary (CHO) cell transfected with OMR, the binding of [H-3]naloxone was displaced by sinomenine in a concentration-dependent manner. This compound also raised the phosphorylation of OMR in these cells. In a tail-flick test, sinomenine produced dose-dependent antinociception in mice, which was dose-dependently inhibited by pretreatment of naloxonazine, a selective OMR antagonist. Long-term pretreatment with sinomenine may delay the analgesic tolerance of morphine. The obtained results suggest that sinomenine has an ability to activate OMR, implicating the potential of sinomenine to be applied in clinic. (C) 2008 Elsevier Ireland Ltd. All rights reserved.
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