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[脑细​​胞示踪剂的化学和药理学方面]

[Chemical and pharmacological aspects of cerebral cellular tracers].

作者信息

Rapin J R, Duterte D, Le Poncin-Lafitte M, Coornaert S, Desplanches G, Bardy A, Askienazy S, Moretti J L, Raynaud C

出版信息

Sem Hop. 1983 Dec 22;59(48):3361-5.

PMID:6318360
Abstract

Among the iodophenylalkylamines studied and labelled with iodine 125 or iodine 123, N-isopropyl-iodo-amphetamin (IAMP) was selected and proposed as tracer for blood flow, a "chemical embolus" having almost 100% extraction in the brain. A new way of obtaining N-isopropyl-p-iodo-amphetamin is proposed and the easily-applied exchange reaction with iodine 125 or 123 gives a product with a radiochemical purity of more than 96% and an unexchanged radioactive iodine content of less than 1%. The pharmacokinetic study of this product in the Wistar rat showed distribution in three compartments and the appearance of a steady state by the fourth minute. The target organs are the lungs, liver and brain. The latter receives 3% of the radioactivity and the autoradiographic study shows that the early distribution in the brain for IAMP closely equals the blood flow as found by a diffusible indicator. In the first hour, the redistribution is very low and at this time although IAMP is proposed for the study of regional blood flow, it does not exactly determine the flow but rather mirrors cell activity.

摘要

在研究的并用碘125或碘123标记的碘苯基烷基胺中,选择了N - 异丙基碘安非他明(IAMP)作为血流示踪剂,它作为一种“化学栓子”在脑中几乎有100%的摄取率。本文提出了一种获得N - 异丙基 - 对碘安非他明的新方法,与碘125或碘123进行的易于应用的交换反应得到了一种放射化学纯度超过96%且未交换的放射性碘含量小于1%的产物。对该产物在Wistar大鼠中的药代动力学研究表明其分布于三个房室,且在第四分钟时出现稳态。靶器官是肺、肝和脑。脑接受3%的放射性,放射自显影研究表明IAMP在脑中的早期分布与通过可扩散指示剂测得的血流非常接近。在第一个小时内,再分布非常低,此时尽管IAMP被用于研究局部血流,但它并不能精确测定血流,而是反映细胞活性。

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