Yang Guang, Gao Jin-xian, Yi Zheng-hong, Yan Lin, Jiang Yuan-Xu
School of Basic Medical Sciences, Ningxia Medical University, Ningxia Engineering & Technology Research Center for Modernization of Hui Medicine, Yinchuan 750004, China.
Yao Xue Xue Bao. 2011 May;46(5):534-8.
.This study is to investigate the analgesic effect produced by intrathecal injection (ith) of oxysophoridine (OSR) and the mechanism of GABAA receptor. Warm water tail-flick test was used to detect the analgesic effect of OSR (12.5, 6.25, and 3.13 mg.kg-1 ith) and to observe the influence of GABA (gamma aminobutyric acid) agonist or antagonist on the analgesic effect of OSR in mice. Immunohistochemistry method were used to detect the influence of OSR (12.5 mg.kg-1, ith) on the GABAARalpha1 protein expression in spinal cord. The results obtained covers that OSR (12.5 and 6.25 mg.kg-, ith) alleviates pain significantly with the warm water tail-flick test (P<0.05, P<0.01), the rate of pain threshold increases by 68.45%; GABA and muscimol (MUS) produces analgesic synergism together with the OSR, picrotoxin (PTX) and bicuculline (BIC) antagonize the analgesic effect of OSR; OSR (12.5 mg.kg-1, ith) significantly increase the positive number of GABAARalpha1 nerve cell in spinal cord (P<0.01) and significantly decrease the average grey levels (P<0.01). In conclusion, OSR intrathecal injection has significant analgesic effect. And GABAA receptor in spinal cord is involved in the analgesic mechanism.
本研究旨在探讨鞘内注射氧化苦参碱（OSR）产生的镇痛作用及GABAA受体的机制。采用温水甩尾试验检测OSR（12.5、6.25和3.13mg·kg-1鞘内注射）的镇痛作用，并观察GABA（γ-氨基丁酸）激动剂或拮抗剂对小鼠OSR镇痛作用的影响。采用免疫组织化学方法检测OSR（12.5mg·kg-1，鞘内注射）对脊髓中GABAARα1蛋白表达的影响。结果表明，OSR（12.5和6.25mg·kg-1，鞘内注射）在温水甩尾试验中显著减轻疼痛（P<0.05，P<0.01），痛阈提高率达68.45%；GABA和蝇蕈醇（MUS）与OSR产生镇痛协同作用，印防己毒素（PTX）和荷包牡丹碱（BIC）拮抗OSR的镇痛作用；OSR（12.5mg·kg-1，鞘内注射）显著增加脊髓中GABAARα1神经细胞的阳性数量（P<0.01），并显著降低平均灰度值（P<0.01）。综上所述，鞘内注射OSR具有显著的镇痛作用。脊髓中的GABAA受体参与了镇痛机制。
