Synthesis and evaluation of a phenylbenzothiazole-based 99mTc(CO)3-radiotracer for possible application in imaging of β-amyloid plaques in Alzheimer’s disease

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• 作者：Drishty Satpati (1)
  Aruna Korde (2)
  H. D. Sarma (3)
  Sharmila Banerjee (1)
  
• 关键词：Amyloid imaging ; Alzheimer’s disease ; Benzothiazole ; [99mTc(CO)3(H2O)3]+
• 刊名：Journal of Radioanalytical and Nuclear Chemistry
• 出版年：2014
• 出版时间：December 2014
• 年：2014
• 卷：302
• 期：3
• 页码：1339-1344
• 全文大小：268 KB
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• 作者单位：Drishty Satpati (1)
  Aruna Korde (2)
  H. D. Sarma (3)
  Sharmila Banerjee (1)
  
  1. Radiopharmaceuticals Chemistry Section, Radiochemistry and Isotope Group, Bhabha Atomic Research Centre, Mumbai, 400 085, India
  2. Isotope Production & Applications Division, Bhabha Atomic Research Centre, Mumbai, India
  3. Radiation Biology and Health Sciences Division, Bhabha Atomic Research Centre, Mumbai, India
  
• ISSN：1588-2780

文摘

The 2-phenyl benzothiazole pharmacophore is known to have high affinity for amyloid beta (Aβ) and is therefore derivatized, to [N-(4-benzothiazol-pyridin-2-yl-methyl-amino)-acetic acid (BTPAA)] for radiolabeling with [99mTc(CO)3(H2O)3]+ precursor. The radiotracer, 99mTc(CO)3–BTPAA is evaluated in vitro and in vivo to determine its binding with the Aβ and ability to cross the blood brain barrier. The radiotracer prepared in >95?% radiochemical yield, showed ~25?% inhibition in presence of thioflavin-T, indicating its specificity towards aggregated Aβ protein. The radiotracer also showed brain uptake of 0.25?±?0.04?% injected dose/g at 2?min post injection, indicating its ability to cross the blood brain barrier.