open access

Vol 11, No 2 (2008)
Published online: 2008-11-05
Submitted: 2012-01-23
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Preparation and evaluation of [61Cu]-thiophene-2-aldehyde thiosemicarbazone for PET studies

Amir R. Jalilian, Mirsaeed Nikzad, Hassan Zandi, Ali Nemati Kharat, Pejman Rowshanfarzad, Mehdi Akhlaghi, Fatemeh Bolourinovin
Nucl. Med. Rev 2008;11(2):41-47.

open access

Vol 11, No 2 (2008)
Published online: 2008-11-05
Submitted: 2012-01-23

Abstract

BACKGROUND: [61Cu]Thiophene-2-aldehyde thiosemicarbazone ([61Cu]TATS) (4) was prepared according to an analogy of carrier copper compound with antitumor activity, for eventual use in PET.
MATERIAL AND METHODS: [61Cu]TATS was prepared using copper-61 acetate and in-house made ligand (TATS) in one step. 61Cu was produced via the natZn(p,x)61Cu nuclear reaction (180 μA, 22 MeV, 3.2 h) followed by a two-step chromatography method (222 GBq of 61Cu2+). [61Cu]TATS preparation was optimized for reaction conditions (buffer concentration and temperature). The tracer was finally administered to normal rats for biodistribution studies.
RESULTS: Total radiolabelling of the tracer took 30 minutes with a radiochemical purity of more than 90% (using HPLC and RTLC) and specific activity of about 250–300 Ci/mmol. The complex was stable in the presence of human serum for an hour. The biodistribution of copper cation and the tracer was checked in wild-type rats for up to 2 hours with significant spleen and lung uptake of the tracer.
CONCLUSIONS: The production of 61Cu via the natZn(p,x)61Cu is an efficient and reproducible method with high specific activity leading to the production and preliminary evaluation of [61,Cu]TATS, a potential PET tracer, was reported.

Abstract

BACKGROUND: [61Cu]Thiophene-2-aldehyde thiosemicarbazone ([61Cu]TATS) (4) was prepared according to an analogy of carrier copper compound with antitumor activity, for eventual use in PET.
MATERIAL AND METHODS: [61Cu]TATS was prepared using copper-61 acetate and in-house made ligand (TATS) in one step. 61Cu was produced via the natZn(p,x)61Cu nuclear reaction (180 μA, 22 MeV, 3.2 h) followed by a two-step chromatography method (222 GBq of 61Cu2+). [61Cu]TATS preparation was optimized for reaction conditions (buffer concentration and temperature). The tracer was finally administered to normal rats for biodistribution studies.
RESULTS: Total radiolabelling of the tracer took 30 minutes with a radiochemical purity of more than 90% (using HPLC and RTLC) and specific activity of about 250–300 Ci/mmol. The complex was stable in the presence of human serum for an hour. The biodistribution of copper cation and the tracer was checked in wild-type rats for up to 2 hours with significant spleen and lung uptake of the tracer.
CONCLUSIONS: The production of 61Cu via the natZn(p,x)61Cu is an efficient and reproducible method with high specific activity leading to the production and preliminary evaluation of [61,Cu]TATS, a potential PET tracer, was reported.
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Keywords

copper-61; radiolabelling; biodistribution; thiophene-2-aldehyde thiosemicarbazone

About this article
Title

Preparation and evaluation of [61Cu]-thiophene-2-aldehyde thiosemicarbazone for PET studies

Journal

Nuclear Medicine Review

Issue

Vol 11, No 2 (2008)

Pages

41-47

Published online

2008-11-05

Bibliographic record

Nucl. Med. Rev 2008;11(2):41-47.

Keywords

copper-61
radiolabelling
biodistribution
thiophene-2-aldehyde thiosemicarbazone

Authors

Amir R. Jalilian
Mirsaeed Nikzad
Hassan Zandi
Ali Nemati Kharat
Pejman Rowshanfarzad
Mehdi Akhlaghi
Fatemeh Bolourinovin

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