氧化槐定碱镇痛作用及其对小鼠中枢GABA_ARα1表达的影响

Analgesic effect of oxysophoridine with intravenous injection andits influence on central GABA_ARα1 receptor in mice

目的研究氧化槐定碱(oxysophoridine,OSR)的镇痛作用及其对小鼠全脑和脊髓GABAA受体表达的影响。方法采用温浴法测定小鼠痛阈,观察OSR(iv)对小鼠热甩尾潜伏期的影响;采用蛋白印迹实验技术(Western blot)检测OSR对小鼠脊髓和脑GABAARα1蛋白表达的影响;采用荧光实时定量PCR方法检测OSR对小鼠脊髓和脑GABAARα1 mRNA表达的影响。结果 OSR(500.0,250.0 mg.kg-1,iv)可明显延长小鼠温浴热甩尾潜伏期(P<0.05,P<0.01),药效可持续60 min以上,最大痛阈提高率可达59.82%。OSR(500.0 mg.kg-1,iv)可使福尔马林致痛小鼠脊髓和脑GABAARα1 mRNA和蛋白表达量均明显升高(P<0.01,P<0.05)。结论 OSR具有明显的镇痛作用,脊髓和脑GABAARα1参与了OSR的镇痛机制。

Aim To study the analgesic effect of oxysophoridine（OSR） and its influence on GABAA receptor expression.Methods The Warm water tail-flick test was used to detect the analgesic effect of OSR（iv）.Western blot method was used to inspect the influence of OSR on the protein expression of GABAARα1 of spinal cord and brain in the formalin test in mice.The Quantitative Real-Time PCR method was used to inspect the influence of OSR on GABAARα1mRNA expression of spinal cord and brain in mice.Results OSR（500.0,250.0 mg·kg-1,iv） could significantly increase the tail-flick latency,and the analgesic effect could last more than 90 min and the maximum rate of pain threshold could be up to 59.82%.OSR（500.0 mg·kg-1,iv）could significantly increase GABAARα1 mRNA and protein expression in spinal cord and brain（P0.01,P0.05） in the formalin test.Conclusions OSR has a significant analgesic effect,GABAA Rα1 receptor of spinal cord and brain is involved in the analgesic mechanism.