目的探讨新型正性肌力活性物PHR0007(三唑并二氢喹啉衍生物)对大鼠动脉血压和心电图的影响和作用机制。方法经股动脉插管连接压力换能器和用针状电极连接标准肢体导联,利用BL-420S生物机能实验系统观察给药前和静脉单用PHR0007(0.1、0.3、1.0μg·kg^-1)或米力农(3.8μg·kg^-1),以及合用PHR0007(0.1μg·kg^-1)和米力农(3.8μg·kg^-1)后1h之内的股动脉血压和肢体标准Ⅱ导联心电图变化。结果与给药前比较,注射PHR0007后0.10-0.75h内收缩压显著提高(P〈0.05)。注射米力农后0.10-0.25h内收缩压也明显增高(P〈0.05)。合用米力农和PHR0007后0.10-0.75h内收缩压虽然升高(P〈0.05),但较单用PHR0007或米力农无明显差异(P〉0.05)。0.1μg·kg^-1 PHR0007使心率减慢(P〈0.05)。不同浓度的PHR0007使QT间期延长(P〈0.05),且在低剂量更加明显。各种处理因素对舒张压和PR间期无显著性影响。结论类似米力农,PHR0007对大鼠具有强心和扩血管作用。
Objective To investigate the effect of PHR0007, a[1,2,4] triazolo[4,3-a] quinoline derivative, on the arterial blood pressure and electrocardiogram in rats. Methods Rats were intravenously administered with PHR0007(0.1,0.3 and 1.0μg·kg^-1) ,or milrinone(3.8μg·kg^-1) ,or in combination of PHR0007(0.1μg·kg^-1) and milrinone (3.8μg·kg^-1). The femoral arterial blood pressure and electrocardiogram were detected with pressure transducer and the standard limb lead Ⅱ which were connected with BL-420S biological function processing system. Results Compared with the pre-treatment (prior to administration), 0.1- 1.0μg·kg^-1 of PHR0007 increased the systolic blood pressure significantly (P 〈 0.05) within the time from 0.10 h to 0.75 h,and a single dose of milrinone increased the systolic blood pressure significantly(P 〈0.05) at the time within 0.10h and 0.25 h. The combination of milrinone and PHR0007 increased the systolic blood pressure significantly ( P 〈 0.05) within 0.10h and 0.75h, which were not significantly different from that of a single dose of PHR0007 or milrinone. 0.1-1.0μg·kg^-1 PHR0007 prolonged the QT interval significantly(P 〈0.05) ,especially at the dose of 0.1μg·kg^-1. All treatments have not altered the diastolic blood pressure, heart rate and PR interval significantly, except for 0.1μg·kg^-1 of PHR0007 which apparently lowered the heart rate( P〈0.05). Conclusions Same as milrinone, PHR0007 presented the positive inotropic and vasodilating functions in rats.