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目的:探讨从蝎毒分离、纯化的多肽(蝎毒五号)的镇痛作用及其镇痛作用机制。方法:通过醋酸扭体法、热板法和甲醛致痛法评价蝎毒五号的药理作用;通过运用纳洛酮拮抗实验,探索蝎毒五号镇痛作用与阿片受体的关系;记录大鼠坐骨神经给药前后动作电位潜的变化情况,探索蝎毒五号对神经传导的影响;通过局部给药,观察小鼠对光热甩尾潜伏期的变化情况,进一步探讨蝎毒五号的镇痛机制。结果:静脉注射蝎毒五号0.6mg/kg、0.3mg/kg和0.15mg/kg均能明显提高小鼠对热板法引起的痛阈值,减少醋酸扭体次数;蝎毒五号0.6mg/kg和0.3mg/kg也能显著降低小鼠对甲醛致痛的第一相和第二相反应。其镇痛作用不能完全被纳洛酮所拮抗。蝎毒五号1.112mg/ml、0.834mg/ml、0.626mg/ml、0.470mg/ml均可明显减小大鼠坐骨神经的动作电位幅度,减慢传导速度,其中蝎毒五号0.470mg/ml还可显著缩短大鼠坐骨神经动作电位时长和去极化时间。在局部作用中,蝎毒五号能延长光热致小鼠甩尾反应潜伏期。结论:蝎毒五号的中枢和外周镇痛作用均较明显,其作用机制可能部分与作用于阿片受体以及阻断神经传导有关。
Objective: To investigate the analgesic effect and analgesic mechanism of peptides isolated and purified from Buthus martensii venom. Methods: The pharmacological effects of scorpion toxin V were evaluated by acetic acid writhing method, hot plate method and formaldehyde induced pain method. By using naloxone antagonistic experiment, the relationship between analgesic effect of scorpion venom V 5 and opioid receptor was explored The potential changes of action potentials before and after sciatic nerve administration in rats were investigated to explore the effect of scorpion toxin V on nerve conduction. The local administration was used to observe the changes of mice’s tail flick latency and to explore the analgesic effects of scorpion toxin V. mechanism. Results: Intravenous injection of Scorpion Poison No. 5 at 0.6mg / kg, 0.3mg / kg and 0.15mg / kg significantly increased the pain threshold caused by the hot plate method and reduced the number of writhing in acetic acid. Scorpion toxin No.5 0.6mg / kg and 0.3 mg / kg also significantly reduced the first and second phase responses in mice induced by formaldehyde. Its analgesic effect can not be completely antagonized by naloxone. Scorpion venom IV 1.112mg / ml, 0.834mg / ml, 0.626mg / ml, 0.470mg / ml can significantly reduce the action potential amplitude of the sciatic nerve in rats, slowing down the conduction velocity, including scorpion toxin V 0.470mg / ml But also significantly shorten the rat sciatic nerve action potential duration and depolarization time. In the local role, Scorpion toxin No. 5 can extend photothermal mouse tail flick reaction latency. CONCLUSION: The analgesic effect of scorpion venison No.5 in the central and peripheral areas is more obvious, and its mechanism may be partly related to the action of opioid receptors and the block of nerve conduction.