摘要
附子有效成分去甲乌药碱（ＤＭＣ）的药理作用以及与肾上腺素能β受体（β－ＡＲ）的关系的研究表明，０．５ｍｇ·ｋｇ－１的ＤＭＣ可使正常小鼠心肌β－ＡＲ轻度上调，与异丙肾上腺素（ＩＳＯ）相比，ＤＭＣ能轻度激动ｃＡＭＰ，使其血浆含量升高，升高的峰值时间在１０ｍｉｎ左右。ＤＭＣ的最小激动量为０．５ｍｇ·ｋｇ－１，最大激动量为５ｍｇ·ｋｇ－１。ＤＭＣ对１２５Ｉ－ＰＩＮ的竞争抑制实验表明，在１×１０－６～１×１０－５ｍｏｌ·Ｌ－１时，ＤＭＣ可抑制１２５Ｉ－ＰＩＮ与β－ＡＲ结合，与心得安比较抑制浓度大４～５个数量级。与ＩＳＯ合并用药观察血浆ｃＡＭＰ浓度变化提示，０．５ｍｇ·ｋｇ－１ＤＭＣ与小剂量（０．１ｍｇ·ｋｇ－１）和较大剂量（１ｍｇ·ｋｇ－１）的ＩＳＯ合用时，既无协同作用，也未见拮抗作用。
The action of higenamine on myocardial beta-adrenergic receptor (β-AR)and plasma cAMP was studied in mice. The results were shown that ip higenamine 0.5 mg· kg-1 caused a slight up-regulation (P<0.05) of myocardial β-AR and increase of plasma cAMP. The peak effect of cAMP was attained at 10 min. The minimal and maximal response in plasma cAMP induced by higenamine were 0.5mg·kg-1 and 5 mg·kg-1 respectively. The action of isoproterenol(0.1～1mg·kg-1) in increasing plasma cAMP level was neither potentiated nor antagonized by higenamine 0.5 mg·kg-1、125Ⅰ-Pindolol can be blocked by higenamine(1×10-6～1×10-5 mol·L-1) in competitive binding experiment of receptor, but the inhibition concentration was greater than that induced by propranolol (1×10-11 ～1×10-10 mol·L-1) (Dept.of Pharmacology, Jiang Shan Hospital, Zhe Jiang Province, 324100)(Research Laboratory of Cell Regulation, Shanghai SecondMedical university, 200025)
出处
《中国药理学通报》
CAS
CSCD
北大核心
1995年第2期113-116,共4页
Chinese Pharmacological Bulletin
