Cheglakov I B, Bochkov V N, Tkachuk V A
Laboratory of Molecular Endocrinology, Institute of Experimental Cardiology, Moscow, Russia.
Arzneimittelforschung. 1997 Mar;47(3):244-7.
The influence of the new calcium antagonist mibefradil (CAS 116666-63-8, Ro 405967) on calcium influx into rabbit smooth muscle cells (VSMC) was studied. Angiotensin II-stimulated divalent cations entry was blocked by mibefradil at micromolar concentrations (1-10 mumol/l). In the same range of concentrations, the antagonist depressed capacitative calcium influx evoked by thapsigargin- and 2,5-di-tert-butylhydroquinone (BHQ)-dependent depletion of internal depots. The ability to block the receptor-mediated pathway of calcium current into VSMC may explain in part the difference between the mode of pharmacological action of mibefradil as compared to other calcium antagonists.
研究了新型钙拮抗剂米贝拉地尔（CAS 116666-63-8，Ro 405967）对兔平滑肌细胞（VSMC）钙内流的影响。米贝拉地尔在微摩尔浓度（1-10 μmol/l）时可阻断血管紧张素II刺激的二价阳离子内流。在相同浓度范围内，该拮抗剂可抑制由毒胡萝卜素和2,5-二叔丁基对苯二酚（BHQ）依赖的内质网钙库耗竭所诱发的容量性钙内流。阻断钙电流进入VSMC的受体介导途径的能力可能部分解释了米贝拉地尔与其他钙拮抗剂相比药理作用模式的差异。
