摘要
采用钙调素非依赖型环核苷酸磷酸二酯酶（ＰＤＥ－Ⅱ）测定方法，观察ＡＰＩ０１３４对ＰＤＥ－Ⅱ的作用。ＡＰＩ０１３４浓度５０ｍｇ·Ｌ－１时明显抑制ＰＤＥ一Ⅱ活性，半效抑制浓度为２１３ｍｇ·Ｌ－１。酶促动力学分析表明：ＡＰＩ０１３４存在时，ＰＤＥ－Ⅱ的Ｋｍ值不变，为１．９２×１０－４ｍｏｌ·Ｌ－１，而Ｖｍａｘ值则随ＡＰＩ０１３４剂量增大而减小，提示ＡＰＩ０１３４为ＰＤＥ－Ⅱ的非竞争性抑制剂。
Using the reactive system of calmodulin-independent cyclic nucleotide phosphodiesterase (PDE-Ⅱ), The effects of API0134 on the activity and kinetic parameters of PDE-Ⅱ were observed. The activity of PDE-Ⅱ was considerably inhibited by API0134 at concentration of more than 50 mg·L-1.and the IC50 was 213 mg· L-1. No change of the Km and decrease of Vmax suggest that the inhibitory effect of API0134 on PDE-Ⅱ activity is incompetitive.
出处
《中国药理学通报》
CAS
CSCD
北大核心
1995年第2期110-112,共3页
Chinese Pharmacological Bulletin
基金
湖北省自然科学基金
