In this section, you can access to the latest technical information related to the FUTURE project topic.

Synthesis and bioevaluation of technetium-99?m / rhenium labeled phenylquinoxaline derivatives as Tau imaging probes

Based on our previous research on the fluorinated phenylquinoxaline scaffold, in this study, different position of N,N-dimethyl amino group, and alkyl linkers with various lengths were introduced into this scaffold to regulate their lipophilicity and binding affinity to Tau. Four novel 99mTc/Re complexes with diethyl iminodiacetate chelator were synthesized and evaluated as Tau imaging tracers in the brain of Alzheimer's disease. Their specific binding to neurofibrillary tangles was verified by in vitro fluorescence staining and further confirmed by the results of immunofluorescent staining on the same brain sections from AD patient and Tg-tau mice. From in vitro binding assay using recombinant Tau aggregates, complex 4.2 with 6-N(CH3)2 and longer carbon chain (n?=?4) displayed the highest affinity (Kd?=?59.95?nM). [99mTc]4.2 was achieved by the ligand exchange reaction between dicarboxylic precursor and [99mTc(CO)3(H2O)]+ intermediate in radiochemical yield over 45%. In vitro biodistribution studies on normal ICR mice revealed that [99mTc]4.2 exhibited moderate initial brain uptake (0.61% ID/g) and more structure optimizations are still required to improve the blood-brain barrier permeability.

» Author: Fan Yang, Kan Wang, Kaixiang Zhou, Bin Dai, Jiapei Dai, Yi Liang, Mengchao Cui

» Reference: 10.1016/j.ejmech.2019.05.065

» Publication Date: 24/05/2019

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