Preparation of [61Cu]-2-acetylpyridine thiosemicarbazone complex as a possible PET tracer for malignancies.
Due to the interesting anti-proliferative properties of copper-thiosemicarbazone complexes, the production of a (61)Cu-labeled thiosemicarbazone, i.e. 2-acetylpyridine thiosemicarbazone (APTS) was investigated. Copper-61 (T(1/2)=3.33 h) was produced via the (64)Zn(p,alpha)(61)Cu nuclear reaction using a natural zinc target irradiated with 22 MeV protons for 500 microAh. The (61)Cu was separated from the irradiated target material by a two-step method and converted to acetate; this yielded a final activity of 222 GBq (6.0 Ci), with a radiochemical yield of >95%. The (61)Cu-acetate was mixed with 2-acetylpyridine thiosemicarbazone for 30 min at room temperature to yield [(61)Cu]APTS with a radiochemical yield of more than 80%. Colorimetric methods showed that residual chemical impurities in the product were below the accepted limits. Radio thin layer chromatography (RTLC) showed a radiochemical purity of more than 99% after C(18) column chromatography. A specific activity of about 370-740 MBq/mmol (10-20 Ci/mmol) was obtained. The stability of the final product was checked in the absence and presence of human serum at 37 degrees C for up to 3 h. The partition coefficient of the final complex was also determined.
Jalilian
A R
AR
Cyclotron and Nuclear Medicine Department, Nuclear Research Center for Agriculture and Medicine, Atomic Energy Organization of Iran, Rajaeeshahr, P.O. Box 31485-498 Karaj, Iran. ajalilian@nrcam.org
Rowshanfarzad
P
P
Sabet
M
M
Shafiee
A
A
D000818:Animals; D003301:Copper Radioisotopes / Q000032:analysis* / Q000737:chemistry*; D004353:Drug Evaluation, Preclinical; D004355:Drug Stability; D006801:Humans; D007553:Isotope Labeling / Q000379:methods; D009369:Neoplasms / Q000000981:diagnostic imaging*; D049268:Positron-Emission Tomography / Q000379:methods*; D019275:Radiopharmaceuticals / Q000032:analysis* / Q000138:chemical synthesis*; D013882:Thiosemicarbazones / Q000032:analysis* / Q000737:chemistry*
D003301:Copper Radioisotopes; D019275:Radiopharmaceuticals; D013882:Thiosemicarbazones; C033836:2-acetylpyridine thiosemicarbazone