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Review
. 2021 Jan 22;9(2):108.
doi: 10.3390/biomedicines9020108.

11C- and 18F-Radiotracers for In Vivo Imaging of the Dopamine System: Past, Present and Future

Affiliations
Review

11C- and 18F-Radiotracers for In Vivo Imaging of the Dopamine System: Past, Present and Future

Michael R Kilbourn. Biomedicines. .

Abstract

The applications of positron emission tomography (PET) imaging to study brain biochemistry, and in particular the aspects of dopamine neurotransmission, have grown significantly over the 40 years since the first successful in vivo imaging studies in humans. In vivo PET imaging of dopaminergic functions of the central nervous system (CNS) including dopamine synthesis, vesicular storage, synaptic release and receptor binding, and reuptake processes, are now routinely used for studies in neurology, psychiatry, drug abuse and addiction, and drug development. Underlying these advances in PET imaging has been the development of the unique radiotracers labeled with positron-emitting radionuclides such as carbon-11 and fluorine-18. This review focuses on a selection of the more accepted and utilized PET radiotracers currently available, with a look at their past, present and future.

Keywords: dopamine; positron emission tomography; radiotracer; receptor; transporter.

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Conflict of interest statement

The author declares no conflict of interest.

Figures

Figure 1
Figure 1
Representative images of specific binding (pixel-by-pixel images of DVR = BP + 1) for three dopaminergic PET radioligands in the striatum of the normal human brain. Note the similarity of the images that are for very different biochemical targets: (A) dopamine D2/3 receptors using [11C]raclopride; (B) vesicular monoamine transporters 2 (VMAT2) using [11C]dihydrotetrabenazine ([11C]DTBZ); (C) the neuronal membrane dopamine transporter DAT using [11C]methylphenidate.
Figure 2
Figure 2
Chemical structures and radiolabeling positions for commonly used dopaminergic PET radiotracers.

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