Sovak M, Barnhart J L, Ranganathan R, Schulze P E, Siefert H M, Speck U
Invest Radiol. 1981 Nov-Dec;16(6):513-6. doi: 10.1097/00004424-198111000-00011.
A new zwitterionic iodinated molecule, 2-[3-(N-ethyl-2-hydroxyethyl) amino-acetamido-2, 4, 6-triiodobenzyl]-butyric acid (RCK-136) was synthesized, and its potential as an oral cholecystopaque was tested. In rats, 15 minutes following intravenous injection, RCK-136 reached maximum biliary concentration; 84% of the dose was excreted into bile. Biliary excretion of RCK-136 elicited a strong choleresis (44 ml of bile flow per mmol compound). Intravenous LD50 in rats averaged 390 mgI/kg. ED50 in rats, intradiencephalic, averaged 1.98 mgI/kg. The average densities of cholecystograms produced in three dogs with iosumetic acid and/or RCK-136 were comparable.
合成了一种新的两性离子碘化分子，即2-[3-(N-乙基-2-羟乙基)氨基-乙酰氨基-2,4,6-三碘苄基]-丁酸(RCK-136)，并测试了其作为口服胆囊造影剂的潜力。在大鼠中，静脉注射后15分钟，RCK-136达到最大胆汁浓度；84%的剂量排泄到胆汁中。RCK-136的胆汁排泄引起强烈的胆汁分泌(每毫摩尔化合物胆汁流量为44毫升)。大鼠静脉注射的半数致死量平均为390毫克碘/千克。大鼠间脑内注射的半数有效量平均为1.98毫克碘/千克。用碘番酸和/或RCK-136对三只狗进行胆囊造影产生的平均密度相当。
