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  • 1 Department of Chemistry, Beijing Normal University Beijing, 100875, P.R. China
  • | 2 Northwest Institute of Nuclear Technology Xi’an ShannXi, 710024, P.R. China
  • | 3 Department of Nuclear Medicine, The PLA General Hospital Beijing, 100853, P.R. China
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Summary  

In order to develop small molecular probes for imaging of Aβ plaques in the brain with Alzheimer’s disease, four benzothiazole derivatives as Aβ probes, 3’-125I-BTA, 3’-125I-CBTA, 3’-125I-BTA-Ac, and 3’-125I-CBTA-Ac were successfully prepared. The four probes displayed the following initial brain uptake: 10.28 %ID/g, 3.62 %ID/g, 3.33 %ID/g and 3.71 %ID/g at 2-minute post iv injection, respectively. The study of quantitative structure-activity relationship (QSAR) indicated that the initial brain uptake was correlated with molecule volume (Vm) and dipole moment (Dp), but the Dp was the main factor. 3’-125I-BTA has the highest initial brain uptake among the four Aβ probes because of the smallest Dp.