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天麻素及天麻甙元作用机理的研究
引用本文:郭正平,谭天秩,钟裕国,吴聪. 天麻素及天麻甙元作用机理的研究[J]. 四川大学学报(医学版), 1991, 0(1)
作者姓名:郭正平  谭天秩  钟裕国  吴聪
作者单位:华西医大核医学科(郭正平,谭天秩),药学院药物化学教研室(钟裕国),药学院药物化学教研室(吴聪)
摘    要:氚标记的天麻甙元衍生物-a-异丁基对羟基苄醇(~3H-天018)作用于中枢苯二氮(艹卓)受体,~(125)I标记的天018仍然作用于该受体。天麻甙元及其衍生物竞争性地抑制~(125)I-天018与苯二氮(艹卓)受体的结合,提示作用于苯二氮(艹卓)受体;天麻素则不能抑制,表明与该受体无相互作用。推测天麻素可能在体内先分解生成天麻甙元,透过血脑屏障,再结合到苯二氮(艹卓)受体而发挥药理效应。

关 键 词:天麻素  天麻甙元  受体分析  天麻甙元衍生物  作用机理

Study of the Mechanism of Gastrodin and Derivatives of Gastrodigenin
Guo Zhengping,Tan Tianzhi,Zhong Yuguo,Wu Cong. Study of the Mechanism of Gastrodin and Derivatives of Gastrodigenin[J]. Journal of Sichuan University. Medical science edition, 1991, 0(1)
Authors:Guo Zhengping  Tan Tianzhi  Zhong Yuguo  Wu Cong
Affiliation:Guo Zhengping;Tan Tianzhi;Zhong Yuguo;Wu Cong Department of Nuclear medicine School of Pharmacy
Abstract:The trititated alpha-isobutyl-hydroxybenzyl alcohol(~3H-G018)was foundto be able to bind benzodiazepine(BZ)receptor on the rat brain membrane. The~(125)I labeled G-018 also had the similarbinding activity with this receptor. In thepresent investigation, we observed thatgastrodigenin and its derivatives inhibitedthe ~(125)I-G018 binding of BZ receptor com-petitively. but no inhibition was observedwith gastrodin. The results suggested thatGastrodigenin was bound to BZ receptor,and otherwise, gastrodin wound have nodirect interaction with BZ receptor.Proba-bly, it might metabolize into gastrodige-nin in vivo, and then got through the bloodbrain barrier and bound to BZ receptor,which mediated its pharmacological effectson the central nervous system.
Keywords:Gastrodin  Gastrodigenin  Derivatives  Receptor binding assay  Mechanism
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