四氢小檗碱衍生物86035对豚鼠心室肌L型钙通道的抑制作用

doi:10.3760/j:issn:0376-2491.2002.01.016

CORC > 北京大学 > 生命科学学院

	四氢小檗碱衍生物86035对豚鼠心室肌L型钙通道的抑制作用; Inhibitory action of CPU86035 on L-type calcium current in single ventricular myocyte of guinea pig
	李春 ; 郭继鸿 ; 刘泰摓
刊名	中华医学杂志
	2002
关键词	膜片钳术细胞钙通道
DOI	10.3760/j:issn:0376-2491.2002.01.016
英文摘要	目的研究氯苄基四氢小檗碱(CPU)86035对豚鼠单个心室肌细胞L型钙通道的抑制作用,分析对L型钙通道相互作用的状态依赖性.方法采用膜片钳全细胞技术,记录不同浓度(50～250 μmol/L)CPU86035作用前后的L型钙电流(ICa.L).结果 (1) CPU86035呈剂量依赖性地抑制L型钙电流,半数抑制浓度(IC50)为75 μmol/L. (2) CPU86035对L型钙电流的抑制依赖于保持电位(HP).HP=-40 mV时,75 μmol/L CPU86035的抑制率为49%±2%,HP=-80 mv时,抑制率为64%±4%.(3) CPU86035作用后,稳态激活曲线右移,V1/2由对照的6.7 mV±1.6 mV变为15.4 mV±0.8 mV.(4) CPU 86035作用后,稳态失活曲线右移,V1/2由对照的-19.1 mV±2.5 mV变为-12.6 mV±2.7 mV.(5) 用药后L型钙通道从失活状态恢复的时间变长.结论 CPU86035对L型钙通道有较强的抑制作用,药物可能主要与通道的静息状态结合.; To investigate the effects of CPU86035, a recently synthesized tetrahydroberberine derivative, on the L-type calcium currents (I(Ca.L)) in single guinea pig ventricular myocytes.The effect of CPU86035 of different concentrations (50 approximately 250 micromomol/L) on I(Ca.L) in enzymatically dispersed single guinea pig ventricular myocytes was investigated by using whole-cell patch-clamp technique.(1) CPU86035 concentration-dependently inhibited I(Ca.L), with the IC50 at 75 micromol/L. (2) The inhibition of CPU86035 on I(Ca.L) was dependent on the holding potential (HP). 75 micromol/L CPU86035 inhibited I(Ca.L) by 49% +/- 2% at HP = -40 mV, and 64% +/- 4% at HP = -80 mV. (3) The homeostatic activation curve of ICa.L shifted to the right toward more positive potentials in the presence of CPU86035, with a V(1/2) of 15.4 mV +/- 0.8 mV compared with that of 15.4 +/- 0.8 mV in the control. (4) The homeostatic inactivation curve of I(Ca.L) shifted to the right toward more positive potentials in the presence of CPU86035, with a V(1/2) of -12.6 mV +/- 2.7 mV compared with that of -19.1 mV +/- 2.5 mV in the control. (5) The recovery from inactivation became slower in the presence of CPU86035.CPU86035 strongly inhibits the calcium channel, probably by binding to the channel in resting stage.; PubMed; 中文核心期刊要目总览(PKU); 中国科学引文数据库(CSCD); 0; 1; 57-60; 82
语种	中文
内容类型	期刊论文
源URL	[http://ir.pku.edu.cn/handle/20.500.11897/261680]
专题	生命科学学院
推荐引用方式 GB/T 7714	李春,郭继鸿,刘泰摓. 四氢小檗碱衍生物86035对豚鼠心室肌L型钙通道的抑制作用, Inhibitory action of CPU86035 on L-type calcium current in single ventricular myocyte of guinea pig[J]. 中华医学杂志,2002.
APA	李春,郭继鸿,&刘泰摓.(2002).四氢小檗碱衍生物86035对豚鼠心室肌L型钙通道的抑制作用.中华医学杂志.
MLA	李春,et al."四氢小檗碱衍生物86035对豚鼠心室肌L型钙通道的抑制作用".中华医学杂志 (2002).