synthesis, radiolabeling and biological evaluation of 99mtc-labeled deoxyglucose derivatives for molecular imaging
Authors
abstract
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 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 ± 0.05towards 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.
similar resources
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]-ECB-DG and [99mTc]-DHP-DG complexes were prepared (96% and 93% radiochemical purities respectively) by using 46 mCi of Na99mTcO4 in 1 mL saline. Radi...
full textSynthesis, 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]-ECB-DG and [99mTc]-DHP-DG complexes were prepared (96% and 93% radiochemical purities respectively) by using 46 mCi of Na99mTcO4 in 1 mL saline. Radi...
full textSynthesis, 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 [(99m)Tc(H2O)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)TcO4 in 1 mL sa...
full textSynthesis and biological evaluation of technetium-99m-labeled deoxyglucose derivatives as imaging agents for tumor.
Three deoxyglucose (DG) derivatives, S-DG, MAG(3)-DG and MAMA-BA-DG, were synthesized and labeled successfully with high labeling yields and high radio-chemical purities. Biodistribution in tumor-bearing mice demonstrated that these three new (99m)Tc-deoxyglucose derivatives showed accumulation in tumor and high tumor-to-muscle ratios. Among them, the (99m)Tc-MAG(3)-DG showed the best character...
full textSynthesis and biological evaluation of 99mTc(CO)3-OH-PP-CS2 for brain receptor imaging
Introduction: 5-HT1A receptor is related with a variety of neuropsychiatric disorders. . In this study a phenolic analogue derived from DWAY [Desmethyl WAY-100635 (N-(2-(1-(4-(2-methoxyphenyl)piperazinyl)-ethyl))-N-(2-pyridinyl) cyclohexanecarboxamide)] is used to design the desired structure of 5-HT1A receptor imaging agents after labeling with [99mTc (CO) 3(H2O) 3] + cor...
full textSynthesis, Radiolabeling, and Biological Evaluation of Peptide LIKKPF Functionalized with HYNIC as Apoptosis Imaging Agent
Introduction: A noninvasive method of detecting exposure of phosphatidylserine (PS) on the external surface of the plasma membrane such as nuclear imaging could assist the diagnosis and therapy of apoptosis related pathologies. The most studied imaging agent for apoptosis is Annexin V so far. Because of limitations of Annexin V other agents have been introduced such as small peptides and molecu...
full textMy Resources
Save resource for easier access later
Journal title:
iranian journal of pharmaceutical researchجلد ۱۲، شماره ۳، صفحات ۲۷۳-۲۸۰
Hosted on Doprax cloud platform doprax.com
copyright © 2015-2023