title: 18F-Labeled 2-Arylquinoline Derivatives for Tau Imaging: Chemical, Radiochemical, Biological and Clinical Features.
abstract: 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. The 18F-labeled tau imaging agents 18F-THK-5351, 18F-T807 (18F-AV-1451), and 18F-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.
authors.forename: Shozo
authors.initials: S
authors.lastname: Furumoto
authors.forename: Tetsuro
authors.initials: T
authors.lastname: Tago
authors.forename: Ryuichi
authors.initials: R
authors.lastname: Harada
authors.forename: Yukitsuka
authors.initials: Y
authors.lastname: Kudo
authors.affiliation: Department of Pharmacology, Tohoku University School of Medicine, 2-1, Seiryo-machi, Aoba-ku, Sendai 980-8575, Japan.
authors.forename: Nobuyuki
authors.initials: N
authors.lastname: Okamura
mesh_terms: D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging* / Q000378:metabolism*; D005462:Fluorine Radioisotopes; D006801:Humans; D049268:Positron-Emission Tomography; D011804:Quinolines / Q000737:chemistry; D019275:Radiopharmaceuticals / Q000737:chemistry; D016875:tau Proteins / Q000378:metabolism*
chemical_list: D005462:Fluorine Radioisotopes; D011804:Quinolines; D019275:Radiopharmaceuticals; D016875:tau Proteins