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[61铜]ATSM作为用于纤维肉瘤成像的正电子发射断层显像(PET)放射性药物的临床前研究。

Preclinical studies of [61Cu]ATSM as a PET radiopharmaceutical for fibrosarcoma imaging.

作者信息

Jalilian Amir R, Rostampour Nima, Rowshanfarzad Pejman, Shafaii Kamaleddin, Kamali-Dehghan Mohsen, Akhlaghi Mehdi

机构信息

Nuclear Medicine Research Group Agricultural, Medical and Industrial Research School (AMIRS), Karaj, Iran.

出版信息

Acta Pharm. 2009 Mar;59(1):45-55. doi: 10.2478/v10007-009-0008-9.

Abstract

[61Cu]diacetyl-bis(N4-methylthiosemicarbazone) ([61Cu] ATSM) was prepared using in house-made diacetyl-bis(N4-methylthiosemicarbazone) (ATSM) ligand and [61Cu]CuCl2 produced via the natZn(p, x)61Cu (180 muA proton irradiation, 22 MeV, 3.2 h) and purified by a ion chromatography method. [61Cu]ATSM radiochemical purity was >98 %, as shown by HPLC and RTLC methods. [61Cu]ATSM was administered into normal and tumor bearing rodents for up to 210 minutes, followed by biodistribution and co-incidence imaging studies. Significant tumor/non-tumor accumulation was observed either by animal sacrification or imaging. [61Cu]ATSM is a positron emission tomography (PET) radiotracer for tumor hypoxia imaging.

摘要

利用自制的双乙酰双(N4-甲基硫代半卡巴腙)(ATSM)配体和通过天然锌(p,x)61铜(180微安质子辐照,22兆电子伏特,3.2小时)产生的[61铜]氯化铜制备了[61铜]双乙酰双(N4-甲基硫代半卡巴腙)([61铜]ATSM),并通过离子色谱法进行纯化。如高效液相色谱法和放射薄层色谱法所示,[61铜]ATSM的放射化学纯度>98%。将[61铜]ATSM注射到正常和荷瘤啮齿动物体内长达210分钟,随后进行生物分布和符合成像研究。通过动物处死或成像观察到明显的肿瘤/非肿瘤蓄积。[61铜]ATSM是一种用于肿瘤缺氧成像的正电子发射断层扫描(PET)放射性示踪剂。

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