摘要
目的:研究2-[(二乙胺)乙酰]-1,2,3,4-四氢-6,7-二甲氧基-1-[1′-(6″-甲氧-2″-萘)乙基]-异喹啉(CPU57)对心脏的作用并与硝苯地平进行比较,着重于其作用机制的研究.方法:测量并记录以下参数:1)豚鼠右心房自发收缩的节律及张力;2)电刺激左心房和右室乳头状肌的等长收缩力.结果:CPU57象经典的钙拮抗剂硝苯地平一样,在0.01-100 μmol·L^(-1)浓度范围内对离体豚鼠心脏具有浓度依赖的负性频率和负性肌力作用,而前者明显弱于后者,且其对心脏的抑制作用比硝苯地平弱.将正常胞外Ca^(2+)浓度从1.5 mmol·L^(-1)降低至0.3或增高至7.5 mmol·L^(-1)可分别增强或减弱CPU57对电刺激左心房收缩的抑制作用.CPU57(1—10 μmol·L^(-1))还抑制CaCl_2所致电刺激左心房的量—效收缩曲线,pD_2′值为4.77.结论:CPU57对豚鼠心脏具有钙拮抗作用.
AIM: To investigate the cardiac actions of 2-[(diethylamino) acetyl]-1 , 2, 3, 4-tetrahydro-6,7-dimethoxyl-l-[1'-(6''-methoxy-2''-naph-thalenyl ) ethyl ]-isoquinoline ( CPU57 ) by comparison with nifedipine and focus on its mechanism of actions. METHOD: The following were measured and recorded: 1) the rate and contraction of spontaneous beating of the guinea pigs right heart atrium, 2) the isometric tension of the electrically stimulated left heart atrium and the right papillary muscles. RESULTS: CPU57 had negative inotropic and negative chronotropic actions in isolated heart of guinea pigs as the typical calcium antagonist, nifedipine. However, CPU57 0. 01 - 100 umol.L-1 produced less cardiac inhibitory potency than nifedipine and had much stronger negative inotropic action than negative chronotropic action. The decrease in external CaCl2 concentration from 1. 5 to 0. 3 mmol.L-1 or increase to 7. 5 mmol .L-1, potentiated or reduced respectively, the inhibitory action of CPU57 on the contraction in paced left heart atrium in normal CaCl2 solution. CPU57 1 - 10umol.L-1 also inhibited contractile response to CaCl2 in paced left heart atrium with pD2' value of 4.77. CONCLUSION: CPU57 has calcium antagonism on the heart of guinea pigs.
出处
《中国药理学报》
CSCD
1995年第3期239-242,共4页
Acta Pharmacologica Sinica
关键词
异喹啉类
硝苯地平
心房
乳头状肌
心肌收缩
isoquinolines
CPU57
nifedipine
heart atrium
papillary muscles
myocardial contraction
heart rate
