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Lignstrazine inhibits high voltage-gated Ca^2+ and TTX-resistant Na^+ channels of primary sensory neuron and thermal nociception in the rat: a study on peripheral mechanism
作者姓名:Bie BH  Chen Y  Zhao ZQ
作者单位:[1]Institute of Shanghai Physiology, Chinese Academy of Sciences, Shanghai 200031, China [2]Institute of Neurobiology, Fu-Dan University, Shanghai 200433, China
摘    要:Objective Ligustrazine, also named as tetramethylpyrazine, is a compound purified from Ligusticum chuanxiong hort and has ever been testified to be a calcium antagonist. The present investigation was to determine the antinociceptive effect of ligustrazine and, if any, the peripheral ionic mechanism involved. Methods Paw withdrawal Latency (PWL) to noxious heating was measured in vivo and whole-cell patch recording was performed on small dorsal root ganglion (DRG) neurons. Results Intraplantar injection of ligustrazine (0.5 mg in 25 μl) significantly prolonged the withdrawal latency of ipsilateral hindpaw to noxious heating in the rat. Ligustrazine not only reversibly inhibited high-voltage gated calcium current of dorsal root ganglion (DRG) neuron in dose-dependent manner with IC50 of 1.89 mmol/L, but also decreased tetrodotoxin (TTX) -resistant sodium current in relatively selective and dose-dependent manner with IC50 of 2.49 mmol/L. Conclusion The results suggested that ligustrazine could elevate the threshold of thermal nociception through inhibiting the high-voltage gated calcium current and TTX-resistant sodium current of DRG neuron .in the rat.

关 键 词:电压  抑制作用  感觉神经  热伤害  小鼠  动物模型
文章编号:1008-0872(2006)02-0079-06
收稿时间:2006-02-04

Ligustrazine inhibits high voltage-gated Ca(2+) and TTX-resistant Na(+) channels of primary sensory neuron and thermal nociception in the rat: a study on peripheral mechanism
Bie BH,Chen Y,Zhao ZQ.Ligustrazine inhibits high voltage-gated Ca(2+) and TTX-resistant Na(+) channels of primary sensory neuron and thermal nociception in the rat: a study on peripheral mechanism[J].Neuroscience Bulletin,2006,22(2):79-84.
Authors:Bie Bi-Hua  Chen Yong  Zhao Zhi-Qi
Affiliation:Institute of Neurobiology, Fu-Dan University, Shanghai 200031, China; Institute of Shanghai Physiology, Chinese Academy of Sciences, Shanghai 200031, China; E-mail: zqzhao@fudan.edu.cn.
Abstract:Objective Ligustrazine, also named as tetramethylpyrazine, is a compound purified from Ligusticum chuanxiong hort and has ever been testified to be a calcium antagonist. The present investigation was to determine the antinociceptive effect of ligustrazine and, if any, the peripheral ionic mechanism involved. Methods Paw withdrawal Latency (PWL) to noxious heating was measured in vivo and whole-cell patch recording was performed on small dorsal root ganglion (DRG) neurons. Results Intraplantar injection of ligustrazine (0.5 mg in 25 mu l) significantly prolonged the withdrawal latency of ipsilateral hindpaw to noxious heating in the rat. Ligustrazine not only reversibly inhibited high-voltage gated calcium current of dorsal root ganglion (DRG) neuron in dose-dependent manner with IC(50) of 1.89 mmol/L, but also decreased tetrodotoxin (TTX) -resistant sodium current in relatively selective and dose-dependent manner with IC(50) of 2.49 mmol/L. Conclusion The results suggested that ligustrazine could elevate the threshold of thermal nociception through inhibiting the high-voltage gated calcium current and TTX-resistant sodium current of DRG neuron in the rat.
Keywords:ligustrazine  nociception  dorsal root ganglion  sodium channel  calcium channel
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