Synthesis, Radiolabeling and Biological Evaluation of 99mTc-labeled Deoxyglucose Derivatives for Molecular Imaging

Two deoxyglucose (dg) derivatives, (α,β)-2-deoxy-2-amino(ethylcarbamate)-d-glucose (ecb-dg) and (α,β)-2-deoxy-2-amino(1,2-dihydroxypropyl)-d-glucose (dhp-dg), were synthesized and radiolabeled successfully with [99mtc(h2o)3(co)3]+ complex. [99mtc]-ecbdg and [99mtc]-dhp-dg complexes were prepared (96% and 93% radiochemical purities respectively) by using 46 mci of na99mtco4 in 1 ml saline. radio-hplc analysis of [99mtc]-ecb-dg at ph = 7.4, revealed that labeling with 99mtc leads to formation of one radiochemical species with tr = 381 second. three radiochemical species, na99mtco4, [99mtc]-dhp-dg and [99mtc(h2o)3(co)3]+ complexes with tr = 342 sec, tr = 567 sec and tr = 1586 sec respectively, were obtained when [99mtc]-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 18f-fdg, [99mtc]-ecb-dg displayed a 2.8-fold reduction in brain uptake (1.7 ± 0.2 versus 0.61% ± 0.09) ,whereas [99mtc]-dhp-dg just showed 1.9-fold reduction in heart uptake (2.2 ± 0.05 towards 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.