β甲基对125碘苯代十五烷酸(125I-BMIPP)的初步动物实验

为了解脂肪酸代谢显像剂 β甲基对12 5碘苯代十五烷酸 (12 5I -BMIPP)在动物体内的分布、清除和代谢干预对其心肌摄取的变化等行为 ,进行了12 5I -BMIPP的动物研究。结果显示 ,禁食SD大鼠心肌对12 5I -BMIPP的摄取高 ,最大吸收值为 5 .70 %/ g ,在心肌中滞留 1h都不变 ,至12 0min心肌摄取仍高达 2 .19± 0 .4 2ID %/ g ;30min心 /血、心 /肝和心 /肺比分别为 3.4 0、2 .6 4和 2 .88;12 5I-BMIPP在肝、肺中的摄取低 ,排泄快 ;甲状腺摄取低 ,至 12 0min ,甲状腺摄取值为 0 .0 2ID %/g ;12 5I-BMIPP与小鼠体内、外血浆蛋白结合稳定 ;异常毒性试验合格 ,每千克小鼠接受的量是人的 5 0 0倍 ;pH为 7.0 0和 7.4 0时的分配系数 (logP)分别为 1.93和 1.6 8;代谢干预研究结果显示 ,葡萄糖胰岛素干预组心肌摄取明显升高 ,与对照组相比差异具有极显著的意义。

Preliminary animal study of β-methyl-ω-p-iodophenyl pentadenoic acid

The biodistribution of 125I-BMIPP in SD rats and the effect of metabolic intervention on myocardial uptake of 125I-BMIPP were reported. The maximal myocardial uptake of 125I-BMIPP in fasted rats was 5.70ID%/g and remained constant during 1h. The myocardial uptake was 2.18ID%/g at 120min postinjection. The ratio of myocardium to blood, myocardium to liver and myocardium to lung at 30min were 3.40, 2.64 and 2.88 respectively. The liver and lung showed a low uptake and rapid clearance of 125I-BMIPP. Toxicity test revealed that the tolerable dose per kg in mice was as high as 500 times that of the recommended dose for clinical application, when the in vivo and in vitro test showed that the binding of 125I-BMIPP to HSA was stable up to 2 h. Partition coefficients (logP) at pH 7.0 and 7.4 were 1.93 and 1.68 respectively. The study of metabolic intervention showed that myocardial uptake of 125I-BMIPP in the glucose-insulin group was significantly increased (P<0.05) than those of the normal control.