Preparation and evaluation of [(61)Cu]-thiophene-2-aldehyde thiosemicarbazone for PET studies.
BACKGROUND
[(61)Cu]Thiophene-2-aldehyde thiosemicarbazone ([(61)Cu]TATS) (4) was prepared according to an analogy of carrier copper compound with antitumor activity, for eventual use in PET.


METHODS
[(61)Cu]TATS was prepared using copper-61 acetate and in-house made ligand (TATS) in one step. (61)Cu was produced via the (nat)Zn(p,x) (61)Cu nuclear reaction (180 mircoA, 22 MeV, 3.2 h) followed by a two-step chromatography method (222 GBq of (61)Cu(2+)). [(61)Cu]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 (61)Cu via the (nat)Zn(p,x) (61)Cu 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.
Jalilian
Amir R
AR
Nuclear Medicine Research Group, Agriculture, Medical and Industrial Research School, Karaj, Iran. ajalilian@nrcam.org
Nikzad
Mirsaeed
M
Zandi
Hassan
H
Kharat
Ali Nemati
AN
Rowshanfarzad
Pejman
P
Akhlaghi
Mehdi
M
Bolourinovin
Fatemeh
F
D000818:Animals; D008168:Lung / Q000000981:diagnostic imaging / Q000378:metabolism*; D008657:Metabolic Clearance Rate; D009928:Organ Specificity; D009942:Organometallic Compounds / Q000737:chemistry* / Q000493:pharmacokinetics*; D049268:Positron-Emission Tomography / Q000379:methods*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000493:pharmacokinetics; D051381:Rats; D013154:Spleen / Q000000981:diagnostic imaging / Q000378:metabolism*; D014018:Tissue Distribution; D051598:Whole Body Imaging / Q000379:methods*
D009942:Organometallic Compounds; D019275:Radiopharmaceuticals