Preclinical studies of [61Cu]ATSM as a PET radiopharmaceutical for fibrosarcoma imaging
[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 μA proton irradiation, 22 MeV, 3.2 h) and purified by a ion chromatography method. [61Cu]ATSM rad...
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Veröffentlicht in: | Acta pharmaceutica (Zagreb, Croatia) Croatia), 2009-03, Vol.59 (1), p.45-55 |
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Zusammenfassung: | [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 μA 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.
[61Cu]diacetil-bis(N4-metiltiosemikarbazon) ([61Cu]ATSM) dobiven je iz liganda diacetil-bis(N4-metiltiosemikarbazona) (ATSM) pripravljenog u vlastitom laboratoriju i [61Cu]CuCl2 dobivenog iz natZn(p, x)61Cu (180 μA protonskim zračenjem, 22 MeV, 3,2 h). [61Cu]ATSM je čišćen ionskom kromatografijom. Prema HPLC i RTLC radiokemijska čistoć a bila je > 98 %. [61Cu]ATSM je davan zdravim glodavcima i glodavcima s tumorom tijekom 210 minuta te je praćena biodistribucija. Žrtvovanjem testiranih životinja te snimanjem primijećena je značajna razlika u akumulaciji [61Cu]ATSM u tumorskom tkivu u odnosu na zdravo tkivo. [61Cu]ATSM je pogodan za dijagnostiku hipoksije tumora pozitron emisijskom tomografijom (PET). |
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ISSN: | 1330-0075 1846-9558 |
DOI: | 10.2478/v10007-009-0008-9 |