Sodium-2 - [(3-butanoylamino-2 4 6-triiodo-phenyl)甲基]butanoate
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Sodium-2 - [(3-butanoylamino-2 4 6-triiodo-phenyl)甲基]butanoate
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- PubMed ID
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20641974 (在PubMed]
- 文摘
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Sodium-2 - [(3-butanoylamino-2 4 6-triiodo-phenyl)甲基]butanoate (tyropanoate钠)是一种口服x射线cholecystographic剂用于援助射线的可视化检测存在胆结石的胆囊胆石病病人(1 - 4)。临床上,这种技术在很大程度上取代超音波,电脑断层扫描(CT);没有对比),核医学技术和仅用于选定的患者(5 - 7)。研究1999 - 2000年报告说,它可能是可行的使用这类药物与螺旋CT胆管造影术(8)。射线成像的胆囊取决于不透明与口服胆囊cholecystographic代理。溶解在肠道内腔,在肠粘膜吸收,运输血液中吸收和排泄由肝脏和胆囊中代理的最终浓度允许x射线成像的胆囊和胆管树(9 - 12)。Cholecystographic代理通常是弱有机酸,包含一个tri-iodinated苯环与碘在位置2,4和6 (2、7、13 - 16)。这类化合物包括碘酸胺酸、碘番酸、丁碘桂酸钠和ipodate。他们的主要化学差异是不同的芳环上取代基位置1和3。取代基的疏水性和亲水性属性决定了水和脂溶性化合物,它必须足够亲脂性的通过胃肠粘膜。缺乏一个取代基位置5允许化合物与血清白蛋白结合,促进肝细胞摄取优惠。 The exact hepatic uptake mechanism is not entirely known. The agent is then metabolized by glucuronide conjugation in the same pathway as bilirubin (17-19). These glucuronide-conjugated compounds are readily excreted into the bile, follow the bile flow to fill up the gallbladder, and then are excreted by the biliary system in the feces. Tyropanoate sodium was first synthesized in1962 as a modification of an earlier cholecystographic agent, iopanoic acid, in an effort to decrease its toxicity (1, 15, 20). Based on the fact that aromatic amino compounds are detoxified in vivo by acetylamino groups, tyropanoate sodium was developed and was different from iopanoic acid, chiefly in the butyrylation of the amine group. Whereas iopanoic acid is insoluble in water, tyropanoate sodium as a salt is soluble in water. The greater aqueous solubility of tyropanoate sodium and the lack of effect of bile acids on its hepatic excretion favor its oral absorption in the fasting state (21). The commercial formulation of tyropanoate sodium contains approximately 57.4% iodine for producing the necessary X-ray attenuation and organ opacification (1, 2, 4). It is no longer marketed in the United States.