双苄基异喹啉类化合物Fs对钙调素拮抗作用的研究

采用钙调素（ＣａＭ）依赖性磷酸二酯酶及丹磺酰标记ＣａＭ，研究了双苄基异喹啉类化合物Ｆｓ对ＣａＭ的拮抗作用。实验结果表明，化合物Ｆｓ能抑制ＣａＭ刺激磷酸二酯酶活性，抑制作用可被过量ＣａＭ完全克服，化合物ＦＳ拮抗作用大于三氟啦嗪，为强的拮抗剂。化合物Ｆｓ在Ｃａ￣（２＋）存在下，可降低丹磺酰钙调素（ＤＮＳ－ＣａＭ）的荧光强度，滴加ＣａＭ，荧光强度逐渐回升，在ＥＧＴＡ条件下，化合物ＦＳ没有作用。实验结果显示：双苄基异喹啉化合物ＦＳ是钙调素拮抗剂，且作用强于三氟啦嗪。

Antagonistic effect of di-benzylisoquinolin compound Fs on calmodulin

The interaction of the di-ben zylisoquinolin compound Fs and calmodulin had been studied.The results showed that the inhibition of phosphodiesterase activity was increased with the rise of compound Fs and was overcomed completely by adding excessive calmodulin.Fluorescence analysis indicated that compound Fs diminished the fluorescence intensity of dansyl-labled calmodulin and the intensity was increased gradually by adding different amounts of calmodulin,showing that the compound Fs is a novel and considerably potent calmod ulin antagonist.Supported by NSFC(NOw in Institute of Medical Biotechnology,Chinese Academy of Medical Science,Beijing 100050)