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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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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.

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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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Authors and Affiliations

  1. Radiopharmaceuticals Chemistry Section, Radiochemistry and Isotope Group, Bhabha Atomic Research Centre, Mumbai, 400 085, India

    Drishty Satpati & Sharmila Banerjee

  2. Isotope Production & Applications Division, Bhabha Atomic Research Centre, Mumbai, India

    Aruna Korde

  3. Radiation Biology and Health Sciences Division, Bhabha Atomic Research Centre, Mumbai, India

    H. D. Sarma

Authors
  1. Drishty Satpati
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  2. Aruna Korde
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  3. H. D. Sarma
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  4. Sharmila Banerjee
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Correspondence to Sharmila Banerjee.

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Satpati, D., Korde, A., Sarma, H.D. et al. Synthesis and evaluation of a phenylbenzothiazole-based 99mTc(CO)3-radiotracer for possible application in imaging of β-amyloid plaques in Alzheimer’s disease. J Radioanal Nucl Chem 302, 1339–1344 (2014). https://doi.org/10.1007/s10967-014-3548-5

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  • DOI: https://doi.org/10.1007/s10967-014-3548-5

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