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。
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.
出处
《华西医科大学学报》
CAS
CSCD
1991年第1期79-82,共4页
Journal of West China University of Medical Sciences
基金
国家自然科学基金
关键词
天麻素
天麻甙元
作用机理
Gastrodin
Gastrodigenin
Derivatives
Receptor binding assay
Mechanism
