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Development and Preliminary Pharmacologic Evaluation of a Zwitterionic Oral Cholecystographic Agent

机译:两性离子口腔胆囊造影剂的开发和初步药理学评价

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A new zwitterionic iodinated molecule, 2-3-(N-ethyl-2-hy-droxyethyl) 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 LD50in rats averaged 390 mgI/kg. ED50in rats, intradiencephalic, averaged 1.98 mgl/kg. The average densities of cholecystograms produced in three dogs with iosumetic acid and/or RCK-136 were comparable.
机译:合成了一种新的两性离子碘化分子2-[3-(N-乙基-2-羟基乙基)氨基-乙酰氨基-2,4,6-三碘苄基]-丁酸(RCK-136),并测试了其作为口腔胆囊酮的潜力。在大鼠中,静脉注射后15分钟,RCK-136达到最大胆汁浓度;84%的剂量被排泄到胆汁中。RCK-136的胆汁排泄引起强烈的胆汁(每mmol化合物44ml胆汁流量)。大鼠静脉LD50平均为390 mgI/kg。ED50在大鼠中,照射脑,平均为1.98 mgl / kg。三只狗用碘己酸和/或RCK-136产生的胆囊造影的平均密度具有可比性。

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