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

doi:10.1016/j.neulet.2008.07.088

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

Research output: Contribution to journal › Article › peer-review

38 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 language	English
Pages (from-to)	209-212
Number of pages	4
Journal	Neuroscience Letters
Volume	443
Issue number	3
DOIs	https://doi.org/10.1016/j.neulet.2008.07.088
Publication status	Published - Oct 10 2008
Externally published	Yes

Keywords

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

ASJC Scopus subject areas

General Neuroscience

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10.1016/j.neulet.2008.07.088

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title = "Activation of opioid μ-receptor by sinomenine in cell and mice",

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.",

keywords = "Antinociception, Mouse, Opioid μ-receptor, Radioligand binding, Receptor phosphorylation, Sinomenine, Transfected cell",

author = "Wang, {Mao Hsien} and Chang, {Cheng Kuei} and Cheng, {Jun Hwa} and Wu, {Hung Tsung} and Li, {Ying Xiao} and Cheng, {Juei Tang}",

note = "Funding Information: We appreciate the kind assistance of Mr. H.H. Chung in some experiments. Thanks are also due to Dr. H. Cheng for a generous supply of sinomenine HCl and Dr. C.W. Tsao for editing. The present study was supported in part by a grant from the National Science Council (NSC 96-2320-B-006-030-MY3) of the Republic of China.",

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AU - Wang, Mao Hsien

AU - Chang, Cheng Kuei

AU - Cheng, Jun Hwa

AU - Wu, Hung Tsung

AU - Li, Ying Xiao

AU - Cheng, Juei Tang

N1 - Funding Information: We appreciate the kind assistance of Mr. H.H. Chung in some experiments. Thanks are also due to Dr. H. Cheng for a generous supply of sinomenine HCl and Dr. C.W. Tsao for editing. The present study was supported in part by a grant from the National Science Council (NSC 96-2320-B-006-030-MY3) of the Republic of China.

PY - 2008/10/10

Y1 - 2008/10/10

N2 - 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.

AB - 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.

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KW - Mouse

KW - Opioid μ-receptor

KW - Radioligand binding

KW - Receptor phosphorylation

KW - Sinomenine

KW - Transfected cell

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

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Keywords

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