Radiosynthesis, In Vitro Characterization, and In Vivo PET Neuroimaging of [18F]F‑4 for Tau Protein: A First-in-Human PET Study

• Published in: ACS chemical neuroscience Vol. 16; no. 6; pp. 1182 - 1189
• Main Authors: Lindberg, Anton, Tong, Junchao, Zheng, Chao, Mueller, Andre, Kroth, Heiko, Stephens, Andrew, Mathis, Chester A., Vasdev, Neil
• Format: Journal Article
• Language: English
• Published: United States American Chemical Society 19.03.2025
• Subjects: Alzheimer Disease - diagnostic imaging; Alzheimer Disease - metabolism; Animals; Brain - diagnostic imaging; Brain - metabolism; Female; Fluorine Radioisotopes; Humans; Male; Neuroimaging - methods; Positron-Emission Tomography - methods; Radiopharmaceuticals - chemical synthesis; Radiopharmaceuticals - pharmacokinetics; Rats; Supranuclear Palsy, Progressive - diagnostic imaging; Supranuclear Palsy, Progressive - metabolism; tau Proteins - metabolism; Tauopathies - diagnostic imaging; Tauopathies - metabolism; tau; fluorine-18; [18F]PI-2620; positron emission tomography; [18F]F-4

[18F]­PI-2620 is a promising radiopharmaceutical for positron emission tomography (PET) imaging of both Alzheimer’s disease (AD) and non-Alzheimer’s disease (non-AD) tauopathies in humans. An array of fluorinated derivatives of the carbazole scaffold of PI-2620 were synthesized and evaluated. In vit...