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 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 language | English (US) |
|---|---|
| Pages (from-to) | 79-84 |
| Number of pages | 6 |
| Journal | Neuroscience Bulletin |
| Volume | 22 |
| Issue number | 2 |
| State | Published - Mar 2006 |
| Externally published | Yes |
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Keywords
- Calcium channel
- Dorsal root ganglion
- Ligustrazine
- Nociception
- Sodium channel
ASJC Scopus subject areas
- Physiology
- Neuroscience(all)
Cite this
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. / Bie, Bi Hua; Chen, Yong; Zhao, Zhi Qi.
In: Neuroscience Bulletin, Vol. 22, No. 2, 03.2006, p. 79-84.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Ligustrazine inhibits high voltage-gated Ca2+ and TTX-resistant Na+ channels of primary sensory neuron and thermal nociception in the rat
T2 - A study on peripheral mechanism
AU - Bie, Bi Hua
AU - Chen, Yong
AU - Zhao, Zhi Qi
PY - 2006/3
Y1 - 2006/3
N2 - 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.
AB - 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.
KW - Calcium channel
KW - Dorsal root ganglion
KW - Ligustrazine
KW - Nociception
KW - Sodium channel
UR - http://www.scopus.com/inward/record.url?scp=33947110416&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=33947110416&partnerID=8YFLogxK
M3 - Article
VL - 22
SP - 79
EP - 84
JO - Neuroscience Bulletin
JF - Neuroscience Bulletin
SN - 1673-7067
IS - 2
ER -