Activation of opioid μ-receptor by sinomenine in cell and mice

Mao Hsien Wang, Cheng Kuei Chang, Jun Hwa Cheng, Hung Tsung Wu, Ying Xiao Li, Juei Tang Cheng

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28 Citations (Scopus)

Abstract

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 μ-receptor (OMR). In Chinese Hamster Ovary (CHO) cell transfected with OMR, the binding of [3H]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.

Original languageEnglish
Pages (from-to)209-212
Number of pages4
JournalNeuroscience Letters
Volume443
Issue number3
DOIs
Publication statusPublished - Oct 10 2008
Externally publishedYes

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Keywords

  • Antinociception
  • Mouse
  • Opioid μ-receptor
  • Radioligand binding
  • Receptor phosphorylation
  • Sinomenine
  • Transfected cell

ASJC Scopus subject areas

  • Neuroscience(all)

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