Schuhmacher J, Matys R, Hauser H, Clorius J H, Maier-Borst W
J Nucl Med. 1983 Jul;24(7):593-602.
We describe the chemical synthesis of an iminodiacetic-acid-substituted tetrabromo-o-cresolphthalein (BP-IDA), which complexes Ga-68 tightly. The liver uptake, bile excretion, and urinary excretion of the complex were examined in rats. Maximum liver uptake reached 60%, and 1-hr cumulative bile excretion was 75% of injected dose. Urinary excretion in rats with ligated common bile duct remained below 1%. Competitive action of exogenous bilirubin on hepatobiliary excretion of the Ga complex was less pronounced than that of bromosulfophthalein. The absolute activity determination of the positron emitter Ga-68, the high accumulation in the liver, the low urinary excretion, and the weak competition from exogenous bilirubin are promising features of this radiopharmaceutical for the quantitative study of hepatobiliary function.
我们描述了一种亚氨基二乙酸取代的四溴邻甲酚酞（BP-IDA）的化学合成方法，该化合物能与镓-68紧密结合。对该配合物在大鼠体内的肝脏摄取、胆汁排泄和尿液排泄情况进行了研究。肝脏摄取最大值达到60%，1小时累积胆汁排泄量为注射剂量的75%。结扎胆总管的大鼠尿液排泄量仍低于1%。外源性胆红素对镓配合物肝胆排泄的竞争作用不如溴磺酞明显。正电子发射体镓-68的绝对活性测定、在肝脏中的高蓄积、低尿液排泄以及外源性胆红素的弱竞争，是这种放射性药物用于肝胆功能定量研究的有前景的特性。
