摘要
本文应用脑依赖于钙调素的环核苷酸磷酸二酯酶,发现慢心律能抑制钙调素激活址该酶活性,IC_(60)=1000μm,而对酶的基础活性无抑制作用,增加反应体系中的钙调素量能减弱慢心律的抑制作用。实验提示慢心律是通过与钙调素相互作用而抑制其对靶酶的激活,这可能与慢心律的两性分子特性有关。
Using Calmodulin (CaM)-dependent cyclic nucleotide Phosphodiesterase we found that Mexiletinum (Mex) could inhibit the activity of the enzyme activated by CaM (IC_(50)=1000μM), but not inhibit the basal activity, and the increase of the amounts of CaM in the reaction system could reduce the inhibition. The results suggest that the inhibition be through the interaction of Mex and CaM. This may relate to the amphipathic nature of Mex.
关键词
慢心律
钙调素
PDE
Mexiletinum, Calmodulin, Cyclic Nucleotide Phosphodiesterase
