Ligustrazine inhibits high voltage-gated Ca2+ and TTX-resistant Na+ channels of primary sensory neuron and thermal nociception in the rat: A study on peripheral mechanism

Bi Hua Bie, Yong Chen, Zhi Qi Zhao

Research output: Contribution to journalArticlepeer-review

10 Scopus citations


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.

Original languageEnglish (US)
Pages (from-to)79-84
Number of pages6
JournalNeuroscience Bulletin
Issue number2
StatePublished - Mar 1 2006


  • Calcium channel
  • Dorsal root ganglion
  • Ligustrazine
  • Nociception
  • Sodium channel

ASJC Scopus subject areas

  • Neuroscience(all)
  • Physiology


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