【摘 要】
：
Bis(7)-tacrine [bis(7)-tetrahydroaminacrine]是一种新型的二聚体乙酰胆碱酯酶抑制剂,由两个tacrine分子通过庚烯键连接而成.实验证明它的药效比tacrine强150倍,抑制乙酰胆碱酯酶的选择性是tacrine的250倍.Tacrine是首先用于缓解治疗老年痴呆症(AD)的乙酰胆碱酯酶抑制剂.Bis(7)-tacrine可以有效逆转大鼠AF64A诱导空间
【机 构】
：
华中科技大学同济医学院神经生物系,武汉430030 中南民族大学神经生物与神经工程所,武汉4300
【出 处】
：
中国神经科学学会第四次会员代表大会暨第七届全国学术会议(The 7th Biennial Meeting and the
论文部分内容阅读
Bis(7)-tacrine [bis(7)-tetrahydroaminacrine]是一种新型的二聚体乙酰胆碱酯酶抑制剂,由两个tacrine分子通过庚烯键连接而成.实验证明它的药效比tacrine强150倍,抑制乙酰胆碱酯酶的选择性是tacrine的250倍.Tacrine是首先用于缓解治疗老年痴呆症(AD)的乙酰胆碱酯酶抑制剂.Bis(7)-tacrine可以有效逆转大鼠AF64A诱导空间记忆缺陷.Bis(7)-tacrine是一种多靶点治疗AD的药物,可作用于酶、神经递质受体和电压门控离子通道等.除了乙酰胆碱酯酶抑制作用外,Bis(7)-tacrine对几种配体门控离子通道也有调制作用,如大鼠海马神经元的GABAAR受体,大鼠三叉神经节神经元的5-HT3R受体,和大鼠海马神经元的NMDAR受体等.本文研究旨在探索bis(7)-tacrine是否如乙酰胆碱酯酶抑制剂tacrine一样也对神经元离子通道具有调制作用及对其动力学参数产生影响.为此我们利用膜片钳技术进行的实验证明：bis(7)-tacrine对DRG神经元电压依赖性Ca2+通道具有明显的抑制作用,较之tacrine的作用强两个数量级左右.
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