A variety of bifunctional chelators have been evaluated for coordination chemistry with 64Cu (t1/2= 12.7 h, I�+=17%, I�-=39%, IEC=43%, Emax=0.656 MeV) for PET imaging. Particularly, 2,2',2'',2'''-(1,4,7,10-tetraazacyclododecane-1,4,7,10-tetrayl)tetraacetic acid (DOTA) and 2,2',2''-(1,4,7-triazonane-1,4,7-triyl)triacetic acid (NOTA)-based macrocyclic bifunctional chelators has been studied for radiolabeling with 64Cu . However, it is known that DOTA complexes radiolabeled with 64Cu sometimes show instability in the in vivo systems. In contrast to that, NOTA has shown better stability in vivo. In this study, three new NOTA derivatives (pentadentate or hexadentate) have been evaluated for labeling efficiency in different reaction conditions varying the temperature and pH. The small structural differences in these NOTA derivatives lead to interesting radiolabelling characteristics. The maximum specific activities were calculated as 14.7 and 4.5 Ci/�mol for the hexadentate NOTA derivatives and <31 Ci/�mol for the pentadentate derivative. The results of radiolabeling efficiency of the new NOTA analogues with 64Cu and in vitro serum stability and in vivo bio-distribution studies for the corresponding NOTA analogues radiolabeled with 64Cu will be discussed.

Study of bifunctional NOTA analogs for <sup>64</sup>Cu radiolabeling

244th National Meeting (2012)

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Study of bifunctional NOTA analogs for 64Cu radiolabeling

Study of bifunctional NOTA analogs for ⁶⁴Cu radiolabeling