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目的α-芋螺毒素LtIA(α-CTX LtIA,LtIA)是从海南产信号芋螺(Conus litteratus)中发现的α3β2乙酰胆碱受体(nAChRs)的特异阻断剂,拟对α-CTX LtIA的镇痛活性进行研究。方法通过小鼠热板和甩尾两种镇痛模型,采用侧脑室给药方式,测试α-CTX LtIA的镇痛效果。结果 0.2 nmol·只~(-1)的剂量侧脑室给药,在甩尾模型中,给药后15 min最大镇痛百分率为37.74%;在热板模型中,给药后60 min最大镇痛百分率达到48.81%。α-CTX LtIA在两种镇痛模型上都表现出良好的镇痛效果。结论α-CTX LtIA通过与乙酰胆碱受体α3β2亚型相互作用表现出良好的镇痛活性,这对LtIA今后作为镇痛药物的研发具有重要指导意义。
The target α-conotoxin LtIA (α-CTX LtIA, LtIA) is a specific blocker of α3β2 acetylcholine receptor (nAChRs) found in Conus litteratus, Pain activity was studied. Methods The analgesic effects of α-CTX LtIA were tested by intracerebroventricular (icv) administration of mouse hot plate and tail flick. Results In the tail flick model, the maximum analgesic percentage was 37.74% at 15 min after the administration of 0.2 nmol • -1 dose. In the hot plate model, the maximal analgesia was 60 min after the administration The percentage reached 48.81%. α-CTX LtIA showed good analgesic effect on both analgesic models. Conclusion α-CTX LtIA shows good analgesic activity through interaction with α3β2 subtype of acetylcholine receptor, which is of great significance for the future development of LtIA as an analgesic.