18F-labeled 2-arylquinoline derivatives for tau imaging: Chemical, radiochemical, biological and clinical features

Shozo Furumoto, Tetsuro Tago, Ryuichi Harada, Yukitsuka Kudo, Nobuyuki Okamura

Research output: Contribution to journalReview articlepeer-review

11 Citations (Scopus)


Alzheimer’s disease is the most common form of dementia among older people. Misfolding and aggregation of proteins (amyloid-β and tau) in the brain is the primary cause of neurodegeneration in the disease. Non-invasive detection of amyloid-β deposition can be realized using positron emission tomography probes, but a proportion of Aβ-positive subjects do not present with cognitive dysfunction, suggesting limitations in assessment using this method. Non-invasive detection of tau deposits in the brain can be used to diagnose, monitor, and predict Alzheimer’s disease progression. Tau positron emission tomography radiolabelled probes such as T807, THK-5117, and PBB3 can image the pathology of the disease in vivo. The18F-labeled tau imaging agents18F-THK-5351,18F-T807 (18F-AV-1451), and18F-RO6958948 are presently under evaluation in clinical studies and clinical trials worldwide. This imaging methodology could be applied to enable preclinical diagnoses and disease-modifying drugs for Alzheimer’s disease. In this review, we provide an overview of the pathology and potential imaging of tau in Alzheimer’s disease, development of a THK series among tau tracers, and the chemical, radiochemical, biological, and clinical features of tau probes.

Original languageEnglish
Pages (from-to)178-185
Number of pages8
JournalCurrent Alzheimer Research
Issue number2
Publication statusPublished - 2017 Feb 1


  • Aggregation
  • Alzheimer’s disease
  • Amyloid-β
  • Brain
  • Positron emission tomography
  • Protein
  • THK series
  • Tau

ASJC Scopus subject areas

  • Neurology
  • Clinical Neurology


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