【摘要】 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LD₅₀:F-CO为1066±138mg/kg,F-OH为1688±276mg/kg。更多还原

【Abstract】 F-co and F-oH were compounds synthesized recently with chemical stra cture closely related to cinnarizine and droperidol. Intravenous admini stration of F-co and F-oH in the dose of 0.5-4mg/kg decreased blood pressure and femoral artery resistance, and slowed heart rate in the anesthetized rabbits. The blood pressure, heart rate, and left ventricular pressure, dp/dt_max were also depressed, by ⅳ F-co and F-oH 0.1-1.0 mgt/kg in the anesthetized dogs. These two compounds decreased the size of myocardial infarction induced by coronary ligation in the rabbits. In isolated central artery of rabbits ear, the aclion of F-co to block voltage-dependent channel was more potens than its a-blocking effects . In the mice, LD50 of F-co and F-oH by oral route were 1066±138mg/kg and 1688±276mg/kg respectively.更多还原