Novel ascorbic acid-resistive nitroxide in a lipid emulsion: An efficient brain imaging contrast agent for MRI of small rodents.

Novel ascorbic acid-resistive nitroxide in a lipid emulsion: An efficient brain imaging contrast agent for MRI of small rodents.
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脂肪乳剂中的新型抗坏血酸硝基氧:一种用于小型啮齿动物 MRI 的有效脑成像造影剂。

DOI:
10.1016/j.neulet.2013.04.044
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发表时间:
2013
期刊:
Neurosci Lett.
影响因子:
--
通讯作者:
Fujii HG.
Fujii HG.
中科院分区:
--
文献类型:
--
作者:
Emoto MC;Yamada KI;Yamato M;Fujii HG.

文献摘要

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氮氧化物最近被用作MRI和EPR成像的氧化还原敏感造影剂。然而,由于抗坏血酸(AsA)等还原剂,氮氧化物的顺磁性在体内迅速降低,限制了它们作为造影剂的使用。本研究开发了一种新合成的抗砷性氮氧化物(2,2,6,6-四乙基哌啶-4- 1-氧基(TEEPONE))的脂质乳状体系配方,并通过磁共振成像(MRI)检测了TEEPONE的体内稳定性。TEEPONE给药后小鼠头部MRI显示TEEPONE具有显著的体内稳定性,是一种血脑屏障(BBB)渗透性氮氧化物。MRI也显示TEEPONE优先定位于小鼠大脑。TEEPONE在小鼠头部的分布可以通过用于溶解TEEPONE的乳液体系中的脂质含量来控制。
Nitroxides have recently been used as redox-sensitive contrast agents for both MRI and EPR imaging. However, the rapid in vivo reduction in paramagnetism of nitroxides due to reductants such as ascorbic acid (AsA) has limited their use as contrast agents. This study developed a formulation of a newly synthesized AsA-resistive nitroxide (2,2,6,6-tetraethylpiperidine-4-one-1-oxyl (TEEPONE)) with a lipid emulsion system and examined the in vivo stability of TEEPONE by magnetic resonance imaging (MRI). MRI of mouse heads after administration of TEEPONE clearly indicated that TEEPONE has a remarkable in vivo stability and is a blood–brain barrier (BBB) permeable nitroxide. MRI also showed that TEEPONE is preferentially localized in the mouse brain. The distribution of TEEPONE in the mouse head can be controlled by the lipid content in the emulsion system used to solubilize TEEPONE.