[γ-氨基丁酸转运体1（GAT-1）下调对氧化苦参碱镇痛作用的影响]

[Effect of down-regulation of GAT-1 on analgesic action of oxysophoridine].

作者信息

Gao Jinxian, Yi Zhenhong, Yang Guang, Yan Lin, Tao Lijun, Gao Shuansheng, Pan Qiuyan, Jiang Yuanxu

机构信息

Department of Pharmacy, People's Hospital of Gansu Province, Gansu 730000, China.

出版信息

Zhongguo Zhong Yao Za Zhi. 2011 Dec;36(23):3315-8.

PMID:22393743

Abstract

OBJECTIVE

To study the effect of GABA transporter (GAT-1) on the analgesic action of oxysophoridine (OSR) in the central nervous system of mice.

METHOD

Hot plate test was used to observe and analyze the effect of gamma aminobutyric acid and the inhibitor of GAT-1 (NO-711) on the analgesic action of oxysophoridine. Real time RT-PCR was used to investigate the influence of OSR on the expression of GAT-1 mRNA induced by formalin in spinal cord and brain of mice.

RESULT

Both GABA (2.0 mg x kg(-1), icv) and NO-711(0.125 mg x kg(-1), icv) enhanced the analgesic action of OSR (32.0 mg x kg(-1), iv) in the hot plate test, and the latencies was markedly increased (P < 0.05, P < 0.01). OSR (500.0 mg x kg(-1), iv) significantly inhibited the expression of GAT-1 mRNA induced by formalin (P < 0.05).

CONCLUSION

GAT-1 was involved in the analgesia effect of OSR and the down-regulation of GAT-1 mRNA enhanced the analgesic effect.

摘要

目的

研究γ-氨基丁酸转运体（GAT-1）对氧化苦参碱（OSR）在小鼠中枢神经系统中镇痛作用的影响。

方法

采用热板试验观察并分析γ-氨基丁酸及GAT-1抑制剂（NO-711）对氧化苦参碱镇痛作用的影响。运用实时逆转录聚合酶链反应（Real time RT-PCR）研究氧化苦参碱对福尔马林诱导的小鼠脊髓和脑中GAT-1 mRNA表达的影响。

结果

在热板试验中，γ-氨基丁酸（2.0 mg·kg⁻¹，脑室内注射）和NO-711（0.125 mg·kg⁻¹，脑室内注射）均增强了氧化苦参碱（32.0 mg·kg⁻¹，静脉注射）的镇痛作用，潜伏期显著延长（P < 0.05，P < 0.01）。氧化苦参碱（500.0 mg·kg⁻¹，静脉注射）显著抑制了福尔马林诱导的GAT-1 mRNA表达（P < 0.05）。