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F-CO和F-OH为参照肉桂嗪和氟呱啶化学结构自行设计合成的化合物。两药0.5～4mg/kgiv对麻醉家兔均剂量依赖性地降低血压(BP)、减慢心率(HR)和降低股动脉阻力(FAR)。对麻醉狗0.1～1.0mg/kg iv,亦可剂量依赖性地降低BP、减慢HR、降低左室内压(LVP)及dP/dtmax。两药均明显缩小家兔结扎冠脉后心肌梗塞范围。离体兔耳动脉标本实验表明F-CO有较弱的α受体阻断作用和较强的电压依赖性钙通道拮抗作用。小鼠口服LD_(50):F-CO为1066±138mg/kg,F-OH为1688±276mg/kg。
F-CO and F-OH are chemical compounds designed according to the chemical structure of cinnarizine and fluocinolide. Both drugs 0.5 ~ 4mg / kgiv dose-dependently lower blood pressure (BP), heart rate (HR) and reduce femoral artery resistance (FAR) in anesthetized rabbits. For anesthetized dogs, 0.1-1.0 mg / kg iv also reduced BP, slowed down HR, decreased left ventricular pressure (LVP) and dP / dtmax in a dose-dependent manner. Both drugs significantly reduce the extent of myocardial infarction in rabbits after ligation of the coronary artery. The experiment of isolated rabbit ear artery showed that F-CO has weaker α-receptor blockade and stronger voltage-dependent calcium channel antagonism. Mice oral LD_ (50): F-CO was 1066 ± 138mg / kg, F-OH was 1688 ± 276mg / kg.