摘要
用大鼠离体胸主动脉环,观察E6 对去甲肾上腺素(NE) 、KCl 和CaCl2 浓度效应曲线及NE 引起的双相收缩的影响。E6 可右移NE、KCl 和CaCl2 浓度效应曲线,并压低最大收缩反应,表现出非竞争性拮抗特性,pD2′分别为4 .63 、4 .32 和3 .78 。对NE 引起的内Ca2 + 依赖性收缩抑制作用较强,对外Ca2 + 依赖性收缩抑制较弱。结果说明,E6 对血管平滑肌上电位依赖性钙通道和受体操纵性钙通道开放有一定的非竞争性抑制作用。
The influences of E6 were studied on the concentration response curves of rat aortic ring constraction evoked by norepinephrine(NE),KCl, CaCl\-2 and on two phases of constraction evoked by NE. E6 moved the concentration response curves to the right, depressed the maximum responses,and showed non competitive antagonism activities. The pD\-\{2\}′ values were 4.63,4.32 and 3.78 respectively.The inhibitory activity of E6 on intracellular Ca\+\{2+\} dependent constraction by NE was more potent than that on extracelluar Ca\+\{2+\} dependent constraction.These results indicated that E6,a calmodulin antagonist, inhibited the opening of potential dependenat Ca\+\{2+\} channel and receptor operated Ca\+\{2+\} channel in a non competitive antagonism way.
出处
《中国药科大学学报》
CAS
CSCD
北大核心
1999年第3期206-208,共3页
Journal of China Pharmaceutical University
关键词
钙调素拮抗剂
E6
动脉环
钙通道
脑缺血
E6
Calmodulin antagonist
Aortic ring
Concentration response curve
Ca\+\{2+\} channel
Non competitive antagonism
