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一种用于心脏和脑部成像的潜在铜放射性药物:铜标记的丙酮醛双(N4-甲基硫代半卡巴腙)

A potential copper radiopharmaceutical for imaging the heart and brain: copper-labeled pyruvaldehyde bis(N4-methylthiosemicarbazone).

作者信息

Green M A

出版信息

Int J Rad Appl Instrum B. 1987;14(1):59-61. doi: 10.1016/0883-2897(87)90162-0.

DOI:10.1016/0883-2897(87)90162-0
PMID:3583756
Abstract

An investigation of the biodistribution of lipophilic copper-64 (half-life = 12.7 h) compounds has been initiated in order to screen potential tracers that could be used to measure regional cerebral and/or myocardial blood flow when labeled with generator-produced 62Cu. The 64Cu complex of pyruvaldehyde bis(N4-methylthiosemicarbazone), [64Cu]Cu-PTSM, was prepared and found to be lipophlic (octanol/saline partition coefficient, log p = 1.97 +/- 0.03). Biodistribution studies following i.v. injection of [64Cu]Cu-PTSM into rats show tracer uptake by the brain and heart. At 1, 5, and 15 min post-injection 3.3, 3.0 and 2.7% of the injected dose was found in the brain. Corresponding brain to blood ratios (per gram) were 3.2, 3.6 and 4.0 respectively. Heart to blood ratios of 7.6, 7.6 and 7.3 were observed at these same time points.

摘要

为了筛选出在用发生器产生的62Cu标记后可用于测量局部脑血流和/或心肌血流的潜在示踪剂,已经开始对亲脂性铜-64(半衰期=12.7小时)化合物的生物分布进行研究。制备了丙酮醛双(N4-甲基硫代半卡巴腙)的64Cu配合物[64Cu]Cu-PTSM,发现其具有亲脂性(辛醇/盐水分配系数,log p = 1.97 +/- 0.03)。对大鼠静脉注射[64Cu]Cu-PTSM后的生物分布研究表明,脑和心脏摄取了示踪剂。注射后1、5和15分钟,在脑中发现的注射剂量分别为3.3%、3.0%和2.7%。相应的脑血比(每克)分别为3.2、3.6和4.0。在这些相同时间点观察到的心血比分别为7.6、7.6和7.3。

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