Ottosson A M, Josefsson M, Ahlner J
Department of Internal Medicine, Central Hospital, Norrköping, Sweden.
Arzneimittelforschung. 1995 Jul;45(7):777-80.
The inhibiting effect of the calcium channel blocker nisoldipine (CAS 63675-72-9, Baymycard, Syscor) on potassium-induced contraction on bovine mesenteric veins and arteries and human peripheral veins was investigated. Nisoldipine inhibited the contraction on bovine mesenteric veins at a significantly lower concentration (1 x 10(-10) mol/l) than nifedipine and glyceryl trinitrate (GTN) (1 x 10(-7) mol/l). When the preparations were preincubated with the drugs, nisoldipine reduced the contraction, measured as area under the curve (AUC), with 47 +/- 8% (mean +/- SEM) and nifedipine with 29 +/- 13% in veins. It was necessary to use an inconsiderably higher concentration of nisoldipine to relax bovine mesenteric arteries contracted by potassium. Preincubation of these arteries with nisoldipine (1 x 10(-7) mol/l) reduced contraction measured as AUC by 46 +/- 10% and preincubation with nifedipine (1 x 10(-7) mol/l) by 77 +/- 3%. Nisoldipine also caused a marked relaxation in human saphenous veins. The introduction of nisoldipine (1 x 10(-8) mol/l) after potassium-induced contraction caused 54 +/- 8% relaxation.
研究了钙通道阻滞剂尼索地平（化学物质登记号63675 - 72 - 9，拜米卡德，西斯科）对钾离子诱导的牛肠系膜静脉和动脉以及人外周静脉收缩的抑制作用。尼索地平抑制牛肠系膜静脉收缩的浓度（1×10⁻¹⁰摩尔/升）显著低于硝苯地平和硝酸甘油（GTN）（1×10⁻⁷摩尔/升）。当制剂与药物预孵育时，尼索地平使静脉收缩（以曲线下面积（AUC）衡量）降低了47±8%（平均值±标准误），硝苯地平降低了29±13%。需要使用高得多的尼索地平浓度才能使由钾离子收缩的牛肠系膜动脉舒张。这些动脉与尼索地平（1×10⁻⁷摩尔/升）预孵育后，以AUC衡量的收缩降低了46±10%，与硝苯地平（1×10⁻⁷摩尔/升）预孵育后降低了77±3%。尼索地平也使人大隐静脉显著舒张。在钾离子诱导收缩后加入尼索地平（1×10⁻⁸摩尔/升）引起了54±8%的舒张。
