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目的 研究新的蝎毒素纯化多肽BmKAS 1及其前级提取物BmK1 3 2对大鼠背根神经节小直径神经元钠通道电流的作用 ,并探讨两者与其外周镇痛作用间的关系。方法 运用全细胞膜片箝技术观察了BmKAS 1和BmK1 3 2对钠电流的作用。结果 10 μg/ml的BmK1 3 2可阻断约 50 %的峰钠电流 ,而 1 6 2 μg/ml的BmKAS 1即可达到相同的阻断效果 ,同时BmKAS 1对钠电流的作用呈现出明显的剂量反应关系。结论 BmKAS 1和BmK1 3 2对钠电流均有较强的抑制作用。鉴于钠通道与损伤所致的外周神经元感觉过敏有关 ,这种抑制作用可能是BmKAS 1和BmK1 3 2外周镇痛作用的机制之一
Objective To study the effect of a novel scorpion toxin purified polypeptide BmKAS 1 and its precursor BmK1 3 2 on sodium channel currents in small diameter neurons of dorsal root ganglion in rats and to explore the relationship between the two and their peripheral analgesic effects. Methods Whole cell patch clamp technique was used to observe the effects of BmKAS 1 and BmK1 3 2 on sodium current. Results BmK1 3 2 at 10 μg / ml blocked about 50% of the peak sodium currents, whereas BmKAS 1 at 162 μg / ml achieved the same blocking effect and the effect of BmKAS 1 on sodium currents was marked Dose-response relationship. Conclusion BmKAS 1 and BmK1 3 2 have a strong inhibitory effect on sodium current. Given that sodium channels are associated with hyperalgesia of peripheral neurons caused by injury, this inhibitory effect may be one of the mechanisms of peripheral analgesia of BmKAS 1 and BmK1 3 2