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放射性碘化1-(二乙氨基丙基)-4-苯基哌嗪:一种潜在的脑显像剂。

Radioiodinated 1-(diethylaminopropyl)-4-phenylpiperazine: a potential brain imaging agent.

作者信息

Hanson R N, Franke L A, Webb N

出版信息

Int J Nucl Med Biol. 1985;12(5):397-400. doi: 10.1016/s0047-0740(85)80011-5.

Abstract

The preparation of radioiodinated 1-(diethylaminopropyl)-4-phenylpiperazine, an analog of HIPDM, and its tissue distribution in rats are described. The precursor undergoes facile electrophilic radioiodination with radionuclides of iodine at the no-carrier-added level to give isolated yields in the 69-85% range. Biodistribution studies indicate that the radiochemical is well extracted by the brain (1.68-1.79% ID) and activity is substantially retained for 4 h (greater than 67%). Brain-to-blood ratios during the 0.25-4.0 h period were 15-23:1. The brain uptake and retention as well as the high brain-to-blood ratios suggest the potential use of this agent for regional cerebral blood flow imaging.

摘要

描述了HIPDM类似物放射性碘化的1-(二乙氨基丙基)-4-苯基哌嗪的制备及其在大鼠体内的组织分布。前体在无载体添加水平下与碘的放射性核素进行简便的亲电放射性碘化反应,得到的分离产率在69 - 85%范围内。生物分布研究表明,该放射化学物质能被脑很好地摄取(1.68 - 1.79%注入剂量),并且活性在4小时内基本保持(大于67%)。在0.25 - 4.0小时期间脑血比为15 - 23:1。脑摄取和保留以及高脑血比表明该试剂在局部脑血流成像方面具有潜在用途。

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