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Journal of Radioanalytical and Nuclear Chemistry

, Volume 302, Issue 3, pp 1339–1344 | Cite as

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

  • Drishty Satpati
  • Aruna Korde
  • H. D. Sarma
  • Sharmila Banerjee
Article

Abstract

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.

Keywords

Amyloid imaging Alzheimer’s disease Benzothiazole [99mTc(CO)3(H2O)3]+ 

Notes

Acknowledgments

The authors are thankful to Dr. Gursharan Singh, Associate Director, Radiochemistry and Isotope group for his encouragement and support towards this work.

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Copyright information

© Akadémiai Kiadó, Budapest, Hungary 2014

Authors and Affiliations

  • Drishty Satpati
    • 1
  • Aruna Korde
    • 2
  • H. D. Sarma
    • 3
  • Sharmila Banerjee
    • 1
  1. 1.Radiopharmaceuticals Chemistry Section, Radiochemistry and Isotope GroupBhabha Atomic Research CentreMumbaiIndia
  2. 2.Isotope Production & Applications DivisionBhabha Atomic Research CentreMumbaiIndia
  3. 3.Radiation Biology and Health Sciences DivisionBhabha Atomic Research CentreMumbaiIndia

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