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

IF 4.1 3区 医学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY
ACS Chemical Neuroscience Pub Date : 2025-03-19 Epub Date: 2025-03-10 DOI:10.1021/acschemneuro.4c00866
Anton Lindberg, Junchao Tong, Chao Zheng, Andre Mueller, Heiko Kroth, Andrew Stephens, Chester A Mathis, Neil Vasdev
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引用次数: 0

Abstract

[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 vitro binding assays with [3H]PI-2620 in human tissues with AD, progressive supranuclear palsy, and corticobasal degeneration, combined with in silico predictions of blood-brain barrier permeability, led to the selection and radiosynthesis of [18F]F-4 as a promising radiotracer. In vivo PET imaging with [18F]F-4 in healthy rats showed brain uptake and kinetics suitable for neuroimaging, similar to those of [18F]PI-2620. A first-in-human PET imaging study in a healthy subject as well as a patient with AD, in comparison with [18F]PI-2620 in the same AD subject, confirmed that [18F]F-4 is an alternative radiopharmaceutical for imaging tau protein.

用于 Tau 蛋白的[18F]F-4 的放射合成、体外表征和体内 PET 神经成像:首次人体 PET 研究。
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来源期刊
ACS Chemical Neuroscience
ACS Chemical Neuroscience BIOCHEMISTRY & MOLECULAR BIOLOGY-CHEMISTRY, MEDICINAL
CiteScore
9.20
自引率
4.00%
发文量
323
审稿时长
1 months
期刊介绍: ACS Chemical Neuroscience publishes high-quality research articles and reviews that showcase chemical, quantitative biological, biophysical and bioengineering approaches to the understanding of the nervous system and to the development of new treatments for neurological disorders. Research in the journal focuses on aspects of chemical neurobiology and bio-neurochemistry such as the following: Neurotransmitters and receptors Neuropharmaceuticals and therapeutics Neural development—Plasticity, and degeneration Chemical, physical, and computational methods in neuroscience Neuronal diseases—basis, detection, and treatment Mechanism of aging, learning, memory and behavior Pain and sensory processing Neurotoxins Neuroscience-inspired bioengineering Development of methods in chemical neurobiology Neuroimaging agents and technologies Animal models for central nervous system diseases Behavioral research
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