Synthesis and imaging of blood‐brain‐barrier permeable nitroxyl‐probes for free radical reactions in brain of living mice
Synthesis and imaging of blood‐brain‐barrier permeable nitroxyl‐probes for free radical reactions in brain of living mice
复制标题
用于活体小鼠脑中自由基反应的血脑屏障可渗透硝酰基探针的合成和成像
DOI：
10.1080/15216549700203051
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发表时间：
1997
期刊：
影响因子：
4.6
通讯作者：
H. Utsumi
中科院分区：
文献类型：
--
作者：
H. Sano;Ken;H. Utsumi
首次合成了三种不同的亲脂性硝基探针，它们具有通过血脑屏障的能力，用于估计活体动物大脑中的自由基反应。其中两种被酯酶水解并留在细胞内。3种探针均具有较高的正辛醇/缓冲分配系数，并在静脉注射后活体小鼠头部的体内ESR光谱中给出2个信号组分。两种组分的ESR参数与溶解于水和脂质相的探针的ESR参数一致。静脉注射后对nilroxyl -证明的ESR - CT成像显示，所有探针均位于头部脑区和颅外区。氮氧基探针的组织分布表明，新合成的亲脂性氮氧基探针比亲水探针具有通过血脑屏障并在脑内积累的能力。
Three different lipophilic nitroxyl‐probes having capability to pass the blood‐brain barrier were, for the ftrst time, synthesized to estimate free radical reactions in brain of living animals. Two of the three were designed to be hydrolyzed by esterase and remain in cell. All 3 probes had high n‐octanol/buffer partition coefficients and gave 2 signal components in in vivo ESR spectra at head of living mice after intravenous injection. The ESR parameters of 2 components agreed with those of probes dissolved in water and lipidic phases. The ESR‐CT imaging on the nilroxyl‐proves after intravenous injection revealed that all probes presented in both encephalon and extracranial region of head. Tissue distribution of the nitroxyl‐probes demonstrated that the newly synthesized lipophilic nitroxyl‐probes had capability to pass the blood‐brain barrier and accumulated in brain than that of hydrophilic probe.