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

摘要

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]-ECB-DG and [^99mTc]-DHP-DG complexes were prepared (96% and 93% radiochemical purities respectively) by using 46 mCi of Na^99mTcO4 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, Na^99mTcO4, [^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.