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目的:探讨一种新型的钙通道拮抗剂HWTX-I(虎纹蜘蛛毒素-I)经硬脊膜外腔用药对大鼠运动性骨关节损伤模型中的抗伤害作用。方法:木瓜蛋白酶踝关节腔内注射制造大鼠踝关节炎性损伤模型,在此模型上分别进行两个剂量组HWTX-I(40μg/kg、80μg/kg大鼠体重)和等体积0.9%生理盐水硬脊膜外腔注射给药。通过检测其关节肿胀度的变化和行为学疼痛评分,观察HWTX-I经硬脊膜外腔用药对该模型的抗伤害作用。结果:40μg/kg和80μg/kg浓度下的HWTX-I均能明显缓解大鼠关节炎性疼痛,并具有剂量依赖性(P<0.05);40μg/kg浓度下的HWTX-I对运动性骨关节损伤的大鼠踝关节肿胀程度影响的差异性不显著。结论:HWTX-I作为一种新型的多肽类钙通道拮抗剂,能够专一性的抑制N-型钙离子通道,阻断伤害性刺激的传导,对实验性骨关节损伤炎性疼痛具有显著的抗伤害性效应。
Objective: To investigate the antinociceptive effects of a new type of calcium channel antagonist HWTX-I administered by the epidural administration to the rat model of osteoarthritis. Methods: Ankle joint injury model was induced by intra-articular injection of papain into the ankle. Rat models of HWTX-I (40μg / kg, 80μg / kg body weight) and 0.9% Saline epidural injection. The antinociceptive effects of HWTX-I on epidural administration were observed by detecting changes in the degree of joint swelling and behavioral pain scores. Results: HWTX-I at 40μg / kg and 80μg / kg significantly relieved arthritis pain in a dose-dependent manner (P <0.05). The effect of HWTX-I at 40μg / kg on exercise- There was no significant difference in the degree of ankle swelling between rats with joint injuries. Conclusion: HWTX-I, as a new type of polypeptide calcium channel antagonist, can specifically inhibit the N-type calcium channel and block the conduction of nociceptive stimuli, and has significant effects on inflammatory pain of experimental bone and joint injury Antinociceptive effect.