[14C]Benzyl acetate is a potential radiotracer for the measurement of glial metabolism in the rat brain
[14C]Benzyl acetate is a potential radiotracer for the measurement of glial metabolism in the rat brain
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DOI：
10.1016/j.nucmedbio.2007.06.011
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发表时间：
2007-11-01
影响因子：
3.1
通讯作者：
Inoue, Osamu
中科院分区：
文献类型：
--
作者：
Momosaki, Sotaro;Hosoi, Rie;Inoue, Osamu
为了研制一种适合测定神经胶质代谢的放射性示踪剂，我们合成了[C-14]乙酸酯的四种不同类型的酯类衍生物，即[C-14]乙酸苯酯、[C-14]对硝基苯乙酸酯、[C-14]2,4-二硝基苯乙酸酯和[C-14]乙酸苄酯（[C-14] BA），并对它们在大鼠体内的药效进行了评价。在这些衍生物中，[C-14]BA在注射后30 s脑摄取最高，比[C-14]醋酸酯本身高23倍以上。[(14) C]BA放射性在大脑中长期保留，而在心脏中放射性迅速清除。[C-14]BA在完整大鼠脑内迅速水解，注射后1 min，放射性标记亲本的含量低于5%。薄层色谱放射化学分析显示，注射后10 min内[C-14]BA在皮质内迅速转化为[C-14]谷氨酰胺和[C-14]谷氨酸。此外，微量注射氟柠檬酸盐（一种选择性胶质毒素）后，[C-14]BA的摄取显著减少。这些结果强烈表明[C-14]， BA可能是一种有用的放射性示踪剂，用于测量完整大鼠脑中的神经胶质代谢。(c) 2007爱思唯尔公司版权所有。
In order to develop a suitable radiotracer for the measurement of glial metabolism, we synthesized four different types of ester derivatives of [C-14]acetate, namely, [C-14]phenyl acetate, [C-14]para-nitrophenyl acetate, [C-14]2,4-dinitrophenyl acetate and [C-14]benzyl acetate ([C-14] BA), and evaluated their potencies in rats. Among the derivatives, the highest brain uptake at 30 s postinjection was observed for [C-14]BA, which was more than 23 times higher than that of [C-14]acetate itself. A long-term retention of [(14) C]BA radioactivity in the brain was observed, whereas rapid clearance of radioactivity was seen in the heart. [C-14]BA was rapidly hydrolyzed in the intact rat brain, and less than 5% of radiolabeled parent was observed 1 min after the injection. Radiochemical analysis using thin-layer chromatography revealed that [C-14]BA was rapidly converted to [C-14]glutamine and [C-14] glutamate in the cortex within 10 min after injection. Furthermore, the uptake of [C-14]BA was significantly decreased following microinjection of fluorocitrate, a selective glial toxin. These results strongly suggest that [C-14], BA may be a useful radiotracer for the measurement of glial metabolism in the intact rat brain. (c) 2007 Elsevier Inc. All rights reserved.