Grandjean E M, Karlaganis G, Noelpp U, Huegli H, Roesler H, Paumgartner G
Scand J Gastroenterol. 1979;14(8):955-60.
The hepatic handling of the bile salt derivative 123I-cholylglycylhistamine has been compared with that of the physiologic bile salt taurocholate in boxer dogs equipped with a Thomas duodenal cannula. After intravenous injection of trace amounts, 123I-cholylglycylhistamine and 14C-taurocholate disappeared from plasma with nearly identical disappearance rate constants. Excellent scintiscans of the liver were obtained with the Anger camera after injection of 3 mCi of 123I-cholylglycylhistamine. Monitoring of radioactivity over a hepatic region of interest revealed rapid uptake of 123I-cholylglycylhistamine by the liver, which reached a maximum 5.7 +/- 0.4 min after injection. The biliary excretion rates of the compounds closely paralleled each other, reaching their maximum within 15 min after injection. Cumulative biliary excretion within 45 min was 58.5 +/- 2.9% and 61.4 +/- 5.0% of the dose for 123I-cholylglycylhistamine and 14C-taurocholate, respectively. Modification of the side chain and gamma-labelling of bile salts may provide scintigraphic agents for the study of the biliary system, which in the behaviour closely resemble the physiologic parent compounds.
在配备了托马斯十二指肠插管的拳师犬中，对胆汁盐衍生物123I-胆酰甘氨酰组胺的肝脏处理过程与生理性胆汁盐牛磺胆酸盐进行了比较。静脉注射微量药物后，123I-胆酰甘氨酰组胺和14C-牛磺胆酸盐从血浆中消失的速率常数几乎相同。注射3毫居里的123I-胆酰甘氨酰组胺后，用安杰尔相机获得了肝脏的优质闪烁扫描图像。对肝脏感兴趣区域的放射性监测显示，肝脏对123I-胆酰甘氨酰组胺的摄取迅速，在注射后5.7±0.4分钟达到最大值。两种化合物的胆汁排泄率彼此密切平行，在注射后15分钟内达到最大值。45分钟内123I-胆酰甘氨酰组胺和14C-牛磺胆酸盐的累积胆汁排泄量分别为给药剂量的58.5±2.9%和61.4±5.0%。胆汁盐侧链的修饰和γ标记可能为研究胆道系统提供闪烁显像剂，其行为与生理性母体化合物非常相似。
