【摘 要】
：
目的：芋螺毒素因其种类繁多,结构新颖,选择性强,疗效确切,并在镇痛、成瘾、麻醉等方面具有极好的应用前景.本实验室发现了结构新颖的αO-芋螺毒素GeXIVA,是迄今α9α10乙
【机 构】
：
海南大学热带生物资源教育部重点实验室,海口市海洋药物重点实验室,海南海口570228
【出 处】
：
第12届生物毒素研究及医药应用学术大会
论文部分内容阅读
目的：芋螺毒素因其种类繁多,结构新颖,选择性强,疗效确切,并在镇痛、成瘾、麻醉等方面具有极好的应用前景.本实验室发现了结构新颖的αO-芋螺毒素GeXIVA,是迄今α9α10乙酰胆碱受体(nAChRs)的活性最强的选择性阻断剂.GeXIVA还是第一个电压依赖性的α9α10nAChRs强阻断剂,其半阻断剂量(IC50)在普通ND96缓冲环境中仅为4.6 nM,在Ba2+-ND96环境中为3.8 nM.GeXIVA在神经痛模型上具有很强的镇痛活性,并可肌肉注射发挥药效,且不成瘾.
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