Synthesis, radiolabeling and biological evaluation of [99m]Tc-labeled deoxyglucose derivatives for molecular imaging

ABSTRACT

Two deoxyglucose [DG] derivatives, [alpha, beta]-2-deoxy-2-amino[ethylcarbamate]-D-glucose [ECB-DG] and [alpha, beta]-2-deoxy-2-amino[1,2-dihydroxypropyl]-D-glucose [DHP-DG], were synthesized and radiolabeled successfully with [[99m]Tc[H[2]O][3][CO][3]][+] complex. [[99m]Tc]-ECB-DG and [[99m]Tc]-DHP-DG complexes were prepared [96% and 93% radiochemical purities respectively] by using 46 mCi of Na[99m]TcO[4] in 1 mL saline. Radio-HPLC analysis of [[99m]Tc]-ECB-DG at pH = 7.4, revealed that labeling with [99m]Tc leads to formation of one radiochemical species with t[R] = 381 second. Three radiochemical species, Na[99m]TcO[4], [[99m]Tc]-DHP-DG and [[99m]Tc[H[2]O][3][CO][3]][+] complexes with t[R] = 342 sec, t[R]= 567 sec and t[R] = 1586 sec respectively, were obtained when [[99m]Tc]-DHP-DG complex evaluated by HPLC. Biodistribution of two complexes were studied on normal mice at 10, 30 and 60 min post-injections. Compared to the [18]F-FDG, [[99m]Tc]-ECB-DG displayed a 2.8-fold reduction in brain uptake [1.7 +/- 0.2 versus 0.61% +/- 0.09], whereas [[99m]Tc]-DHP-DG just showed 1.9-fold reduction in heart uptake [2.2 +/- 0.05towards 1.16 +/- 0.10] at 1 h post-injection.On the basis of our results, it seems that ECB-DG and DHP-DG analogues could be used as brain and heart imaging agent respectively