Fatty-acyl iminopolycarboxylates: lipophilic bifunctional contrast agents for NMR imaging.
Fatty-acyl iminopolycarboxylates: lipophilic bifunctional contrast agents for NMR imaging.
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脂肪酰亚氨基多羧酸盐：用于核磁共振成像的亲脂性双功能造影剂。
DOI：
10.1002/mrm.1910220107
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发表时间：
1991
影响因子：
3.3
通讯作者：
Elgavish,GA
中科院分区：
文献类型：
--
作者：
Kim,SK;Pohost,GM;Elgavish,GA
以双(羟乙基)乙二胺为原料，经烷基化、酰化、催化氢化反应合成了新的脂肪酰基对比剂N3−2‘-肉豆蔻酰氧乙基-N6-−2’-羟乙基-1，8-二氧基三乙四胺-N，N，N‘，N’-四乙酸三乙酯(MHE-DTTA)和N3，N6-二(2‘-肉桂酰氧乙基)-1，8-二氧基三乙四胺-N，N，N’，N‘-四乙酸氢化(总收率36-46%)。将1：1的配体MHE-DTTA和BME-DTTA的Gd络合物掺入脂质体中，测定了它们的体外驰豫活性。在0.23T和0.47T下，两种试剂的弛豫度基本相同，均大于Gd~(3+)水离子、Gd(EDTA)和Gd(DTPA)。这两种试剂的弛豫度从低到高依次增大，表现出正的磁场依赖关系。这是有利的，因为高场(B0>；0.5T)核磁共振成像仪器的广泛使用。Gd(MHE-DTTA)和Gd(BME-DTTA)的稳定常数(LogK)分别为15.27±2.21和16.78±0.36。两种化合物的LD_(50)均为0.2 mmol/kg。这些稳定性和LD50的下限表明这些试剂在体内应用是可能的。©1991学术出版社，Inc.
New fatty‐acyl contrast agents,N3−2′‐myristoyloxyethyl‐N6−2′‐hydroxyethyl‐1, 8‐dioxotriethylenetetraamine‐N, N, N′, N′‐tetraacetic acid (MHE‐DTTA) andN3,N6‐bis (2′‐myristoyloxyethyl)‐1, 8‐dioxo‐triethylenetetraamine‐N, N, N′, N′‐tetraacetic acid (BME‐DTTA) were prepared by sequential alkylation, acylation, and catalytic hydrogenation from bis(hydroxyethyl)‐ethylenediamine with satisfactory yields (overall 36–46%). The 1:1 gadolinium complexes of the ligands MHE‐DTTA and BME‐DTTA were incorporated into liposomes and their relaxivitiesin vitrowere determined. The relaxivities of both agents were similar and were greater than those of Gd3+aquoion, Gd(EDTA), and Gd(DTPA) at both 0.23 T and 0.47 T. The relaxivities of these two agents increased from the lower to the higher magnetic field, indicating a positive field dependence. This is advantageous because of the widespread use of high‐field (B0> 0.5 T) NMR imaging instruments. Stability constants (logK) of Gd(MHE‐DTTA) and Gd(BME‐DTTA) were found to be 15.27 ± 2.21 and 16.78 ± 0.36, respectively. LD50of both compounds was >0.2 mmol/kg. These stabilities and lower limits of LD50indicate the possiblein vivoapplication of these agents. © 1991 Academic Press, Inc.