【摘要】 Nisoldipine 10μg/kg明显缩小家兔心肌梗塞范围,3μg/kg明显降低麻醉狗血压及左室内压,减慢心率,增加冠脉血流量及冠状窦血氧含量;1,3,10μg/kg降低麻醉狗冠脉及椎动脉阻力强于股动脉阻力。1～10μg明显增加离体豚鼠心脏冠脉沉量,抑制心肌收缩振幅,大剂量则减慢心率。2.6×10^-10～1×10^-8M非竞争性对抗KCl收缩家兔离体主动脉条反应,但不影响去甲肾上腺素所致收缩反应。nisoldipine抑制Cacl₂所致离体兔耳血管收缩反应的IC₅₀为1.7×10^-11M,而抑制去甲肾上腺素收缩反应的JC₅₀为4.0×10^-4M。小鼠灌胃LD₅₀为292±32mg/kg。更多还原

【Abstract】 Nisolipine （NS, 10μg/kg） reduced the size of myocardial infarction induced by coronary artery ligation in rabbits. The blood pressure, LVP and heart rate were depressed, while coronary blood flow and oxygen content of coronary sinus blood were increased by NS 3 μg/kg in the anesthetized dogs. A given quantity of NS （1, 3 or 10 μg/kg） reduced the resistance of vascular beds, these effects were more potent in the coronary and vertebral arteries than in the femoral arteries. NS（1-10 μg/kg） increased the coronary flow, diminished the intensity of heart contraction and rate in the isolated perfused guinea pig’s heart. In rabbit’s isolated aortic strips,NS(2.6×10^-10—1×10^-8M)uncompetitively antagonized the response induced by KCl, not by noradrenaline. In isolated central arteries of rabbit’s ear, NS inhibited the vasoconstriction induced by CaCl₂ and noradrenaline, the IC₅₀ was 1.7×10^-11 M and 4.8×10^-4 M respectively. LD₅₀ of NS by stomach tube in the mice was 292±32 mg/kg.更多还原