POLYIODINATED TRIGLYCERIDE ANALOGS AS POTENTIAL COMPUTED-TOMOGRAPHY IMAGING AGENTS FOR THE LIVER
POLYIODINATED TRIGLYCERIDE ANALOGS AS POTENTIAL COMPUTED-TOMOGRAPHY IMAGING AGENTS FOR THE LIVER
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DOI：
10.1021/jm00004a010
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发表时间：
1995-02-17
影响因子：
7.3
通讯作者：
COUNSELL, RE
中科院分区：
文献类型：
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作者：
WEICHERT, JP;LONGINO, MA;COUNSELL, RE
合成了一系列2-油酰基1，3-双[omega-（3-氨基-2，4，6-三碘苯基]）链烷酸甘油酯，用碘-125进行放射性碘标记，乳化，并评价其选择性定位于肝脏的能力，以作为计算机断层扫描中的肝造影剂。所有7个类似物显示快速肝脏摄取，其中65和78%之间的注射剂量在肝脏中积累了30分钟。肝脏值范围从46至93%注射后3小时，这对应于肝脏与血液的比例范围从21至450。此外，放射性从肝脏中的后续消除与烷基链长度几乎呈线性关系。具有较长烷基链长度的类似物比其较短链对应物更快地从肝脏中消除。由于它们与天然存在的甘油三酯的生化相似性，这些新的类似物可能被证明不仅可用于局灶性肝脏病变的高分辨率解剖成像，而且可用于评估已知影响肝功能和生物化学的各种弥漫性疾病。
A series of glyceryl 2-oleoyl 1,3-bis[omega-(3-amino-2,4,6-triiodophenyl]) alkanoates was synthesized, radioiodinated with iodine-125, emulsified, and evaluated for their ability to selectively localize in the liver for potential use as hepatographic agents in computed tomography. All seven analogs displayed rapid liver uptake wherein between 65 and 78% of the injected dose accumulated in the liver by 30 min. Liver values ranged from 46 to 93% 3 h after injection which corresponded to liver to blood ratios ranging from 21 to 450. Moreover, subsequent elimination of radioactivity from the liver was nearly linear with respect to alkyl chain length. Analogs with longer alkyl chain length were eliminated from the liver more rapidly than their shorter chain counterparts. Because of their biochemical similarities to naturally occurring triglycerides, these novel analogs may prove useful not only for high-resolution anatomic imaging of focal liver lesions, but also for evaluating a variety of diffuse diseases known to affect hepatic function and biochemistry.