间硝苯地平对DOCA－salt高血压大鼠肥厚心肌膜碎片二氢吡啶结合位点的影响  

EFFECTS OF M-NIFEDIPINE ON DIHYDROPYRIDINE BINDING SITES IN HYPERTROPHIED LEFT VENTRICULAR CELL MEMBRANES FROM DEOXYCORTICOSTERONE ACETATE-SALT HYPERTENSIVE RATS

作　　者：徐毅[1] 饶曼人[1] 

机构地区：[1]南京医科大学心血管药理研究室,湖南医科大学心血管生理研究室

出　　处：《药学学报》1996年第5期333-339,共7页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金

摘　　要：用ＤＯＣＡ－ｓａｌｔ高血压大鼠心肌肥厚模型，观察间硝苯地平（ｍ－Ｎｉｆ）对肥厚心肌膜碎片二氢吡啶（ＤＨＰ）结合位点的影响。结果显示：预防或治疗性给予ｍ－Ｎｉｆ（２０ｍｇ·ｋｇ￣（－１）·ｄ￣（－１））１２或９周，血压降低，心室重和心肌线粒体钙含量减少，且肥厚心肌ＤＨＰ结合位点密度显著降低（４５０±２５，４６２±３６ｆｍｏｌ·ｍｇ￣（－１）ｖｓ８３６±４７ｆｍｏｌ·ｍｇ￣（－１）ｐｒｏｔｅｉｎ，Ｐ＜０．００１）。提示：ｍ－Ｎｉｆ预防和逆转ＤＯＣＡ－ｓａｌｔ高血压大鼠心肌肥厚的作用可能与其减少肥厚心肌ＤＨＰ结合位点密度和血压降低有关。m-Nifedipine(m-Nif 20 mg·kg-1·d-1 ig)was administered orally to male deoxvcorti-costerone-acetate-salt(DOCA)hypertensive rats for 9 or 12 wk,the affinity and density of dihydropyridines(DHP)binding sites in the membranes of left ventricle(LV)were investigated,Treatment with m-Nif,whether for prevention(6 wk postoperation)or regression(9 wk postoperation)lowered systolic blood ptessure,decreased the weight of left ventricle and the Ca2+ concentration in mitochondria in hypertrophied LV, The density(Bmax)and the total number of DHP binding sites in hypertrophied LV were also markedly decreased(450±25, 462±36 fmol· mg-1 vs 836±47 fmol·mg-1 protein, P<0.001).There was no difference between groups in constant(KD)values of DHP binding sites,These results indicate that m-Nif prevented and regressed cardiac mass in DOCA hypertensive rats through mechanisms that may be associated with their density of DHP binding sites and control of blcod pressure.

关 键 词：间硝苯地平 心肌肥厚 结合位点 二氢吡啶 

分 类 号：R542.205[医药卫生—心血管疾病]