Masumiya H, Tanaka Y, Tanaka H, Shigenobu K
Department of Pharmacology, Toho University School of Pharmaceutical Sciences, Funabashi, Chiba, Japan.
Pharmacology. 2000 Aug;61(2):57-61. doi: 10.1159/000028381.
The effects of aranidipine, a novel dihydropyridine Ca(2+) channel antagonist, on membrane currents in guinea pig ventricular myocytes and on action potentials in rabbit sinoatrial node tissue were examined. In myocytes, aranidipine (10 nmol/l to 1 micromol/l) concentration-dependently decreased T-type and L-type Ca(2+) currents. Aranidipine (1 micromol/l) had little effect on K(+) currents. In the sinoatrial node, 0.1 micromol/l aranidipine increased cycle length, and decreased +V(max) and the slope of the phase 4 depolarization. Thus, inhibition of both T-type and L-type Ca(2+) currents by aranidipine may partly explain its potent negative chronotropic activity.
研究了新型二氢吡啶类钙(Ca2+)通道拮抗剂阿雷地平对豚鼠心室肌细胞膜电流及兔窦房结组织动作电位的影响。在心肌细胞中,阿雷地平(10 nmol/L至1 μmol/L)浓度依赖性地降低T型和L型钙电流。阿雷地平(1 μmol/L)对钾电流几乎无影响。在窦房结中,0.1 μmol/L阿雷地平可延长周期长度,降低最大上升速率(+Vmax)及4期去极化斜率。因此,阿雷地平对T型和L型钙电流的抑制作用可能部分解释了其强大的负性变时活性。