Cu-64-pyruvaldehyde-bis-(N4-methylthiosemicarbazide) or Cu-64-PTSM as tracer for brain positron emission tomography

Synthesis of pyruvaldehyde-bis-(N4-methylthiosemicarbazide) (PTSM), used for medical investigation and diagnosis, has been carried out in our Radiopharmaceutical Division in C.A.E. (Ezeiza Atomic Center). PTSM has been obtained introducing modifications to a previous synthesis published by H.G. Petering. (M.P. 236-238 degrees C). TLC, HPLC and IR spectrum controls have been performed. Cu-64 can be obtained by the Cu-63(n,α) and Zn-64(n,p) reactions. This last reaction has been chosen for the production in the RA-3 reactor since it leads to Cu-64 of high specific activity. Two different assays have been performed to obtain the chelate PTSM-Cu-64. The first one has been obtained by buffering the Cu-64 to pH 3-4; adding the PTSM solution to ethanol. The second assay has been carried out by buffering the Cu-64 solution with sodium acetate 3M and adding 100 μl of PTSM solution. Biodistribution studies have been carried out on NIH and rats showing a brain uptake of 4%, 30 minutes after injection. Thus, PTSM-Cu-64 proves a good brain diagnosis agent. (author). 1 ref