Xi T, Rao M R
Department of Cardiovascular Pharmacology, Nanjing Medical University, China.
Zhongguo Yao Li Xue Bao. 1996 May;17(3):235-8.
To study the effects of menidipine (Men) on the affinity and density of dihydropyridines (DHP) binding sites in the cell membranes of left ventricle (LV) and brain in elderly renovascular hypertensive rats (RVHR) with LV hypertrophy.
Renovascular hypertension was produced by clipping the left renal artery in 20-month-old rats. The affinity and density of DHP binding sites in the cell membranes of LV and brain were assessed by radioligand assay.
Men (20 mg.kg-1.d-1 ig for 9 wk) decreased markedly the systolic blood pressure and the LV weight (P < 0.01). Though not affecting the density of DHP receptor (Bmax), Men markedly decreased the total number of DHP binding sites in hypertrophied LV (from 5.95 +/- 0.62 to 4.0 +/- 1.1 pmol.LV). Men also reduced Bmax of DHP binding sites in the thalamus (from 522 +/- 27 to 371 +/- 24 pmol/g protein) and hippocampus (from 498 +/- 26 to 332 +/- 32 pmol/g protein).
Men reversed the LV hypertrophy from renovascular hypertension accompanied with reduced total number of DHP binding sites in the cell membranes of LV and Bmax of the cell membranes of thalamus and hippocampus from elderly LV hypertrophied rats.
研究尼群地平(Men)对老年肾血管性高血压大鼠(RVHR)左心室肥厚时左心室(LV)和脑细胞膜中二氢吡啶(DHP)结合位点亲和力和密度的影响。
通过夹闭20月龄大鼠的左肾动脉制备肾血管性高血压。采用放射性配体分析法评估左心室和脑细胞膜中DHP结合位点的亲和力和密度。
尼群地平(20mg·kg-1·d-1灌胃9周)显著降低收缩压和左心室重量(P<0.01)。尼群地平虽不影响DHP受体密度(Bmax),但显著降低肥厚左心室中DHP结合位点总数(从5.95±0.62降至4.0±1.1pmol/LV)。尼群地平还降低了丘脑(从522±27降至371±24pmol/g蛋白)和海马体(从498±26降至332±32pmol/g蛋白)中DHP结合位点的Bmax。
尼群地平可逆转老年左心室肥厚大鼠肾血管性高血压所致的左心室肥厚,同时降低左心室细胞膜中DHP结合位点总数以及丘脑和海马体细胞膜中DHP结合位点的Bmax。