Journal of Radiopharmaceuticals and Molecular Probes (대한방사성의약품학회지)

Korean Society of Radiopharmaceuticals and Molecular Probes (대한방사성의약품학회)
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Review of the chemistry of first-generation Tau PET tracers

  • Farag, Ahmed Karam (RI Translational Research Team, Division of Applied RI, Korea Institute of Radiological and Medical Sciences (KIRAMS)) ;
  • Im, Changkeun (RI Translational Research Team, Division of Applied RI, Korea Institute of Radiological and Medical Sciences (KIRAMS)) ;
  • Kang, Choong Mo (RI Translational Research Team, Division of Applied RI, Korea Institute of Radiological and Medical Sciences (KIRAMS)) ;
  • Lee, Yong Jin (Division of Applied RI, Korea Institute of Radiological and Medical Sciences (KIRAMS))
  • Received : 2020.06.15
  • Accepted : 2020.06.26
  • Published : 2020.06.30
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Abstract

Alzheimer's disease (AD) is one of the challenging conditions that have no cure, yet early diagnosis can help to control the disease. PET imaging of tau has several advantages, such as being a noninvasive, safe diagnostic technique that correlates directly with the disease progression. Many tau tracers have been reported to date; however, the chemical scaffolds of them fall in a narrow chemical window, and none was approved yet as none is entirely selective and sensitive to tau. These problems are being solved as new tracers emerge constantly. In this report, the first-generation tau tracers such as [11C]PBB3, 2-arylquinoline (THK) series, [18F]T808, and [18F]AV-1451 ([18F]T807) are reviewed from an organic and radiochemistry perspective; thus the most effective chemical approach to synthesize these tracers is discussed. This would help to design novel tracers which can meet the challenges faced by the current tracers.

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References

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