TY - CHAP
T1 - PET and SPECT imaging of the central dopamine system in humans
AU - Booij, Jan
AU - van Wieringen, Jan-Peter
AU - van de Giessen, Elsmarieke
AU - Knol, Remco J. J.
AU - Finnema, Sjoerd J.
PY - 2020/9/29
Y1 - 2020/9/29
N2 - The neurotransmitter dopamine plays a role in many different functions of the human brain, ranging from psychomotor planning to cognition. This short review addresses which parts of the dopamine system can be imaged quantitatively in the living human brain using positron-emission tomography (PET) or single-photon emission computed tomography (SPECT). Nowadays, imaging of the nigrostriatal dopaminergic pathway in humans can be performed quantitatively using radiotracers like the aromatic amino acid decarboxylase (AADC) substrate [18F]FDOPA, vesicular monoamine transporter 2 (VMAT-2) radioligands derived from tetrabenazine or PET/SPECT radioligands that bind to the dopamine transporter (DAT). Using PET, also several other dopaminergic projection pathways (e.g. mesocortical projections) can be assessed in humans. Several antagonist PET radioligands for the dopamine D1 receptor have been developed successfully. In addition, well-validated antagonist PET and SPECT radioligands are available for imaging of dopamine D2 and dopamine D3 (D2/3) receptors in the living human brain. Also agonist PET radioligands for the dopamine D2/3 receptors have become available, which afford the opportunity to evaluate the existence of the high-affinity state of these receptors in vivo. These agonist radiopharmaceuticals may also prove more sensitive to changes in dopamine concentrations (e.g. induced by the dopamine releaser amphetamine). Finally, selective antagonist PET radioligands for the dopamine D4 receptor have recently been synthesized and evaluated successfully in small laboratory animals, although these radioligands have not yet been reported as applied in human subjects. In conclusion, after almost four decades of research, several relevant parts of the central dopamine system can be assessed quantitatively in the living human brain using PET or SPECT. Future studies may include application of agonist radioligands and more dopamine receptor subtype selective radioligands.
AB - The neurotransmitter dopamine plays a role in many different functions of the human brain, ranging from psychomotor planning to cognition. This short review addresses which parts of the dopamine system can be imaged quantitatively in the living human brain using positron-emission tomography (PET) or single-photon emission computed tomography (SPECT). Nowadays, imaging of the nigrostriatal dopaminergic pathway in humans can be performed quantitatively using radiotracers like the aromatic amino acid decarboxylase (AADC) substrate [18F]FDOPA, vesicular monoamine transporter 2 (VMAT-2) radioligands derived from tetrabenazine or PET/SPECT radioligands that bind to the dopamine transporter (DAT). Using PET, also several other dopaminergic projection pathways (e.g. mesocortical projections) can be assessed in humans. Several antagonist PET radioligands for the dopamine D1 receptor have been developed successfully. In addition, well-validated antagonist PET and SPECT radioligands are available for imaging of dopamine D2 and dopamine D3 (D2/3) receptors in the living human brain. Also agonist PET radioligands for the dopamine D2/3 receptors have become available, which afford the opportunity to evaluate the existence of the high-affinity state of these receptors in vivo. These agonist radiopharmaceuticals may also prove more sensitive to changes in dopamine concentrations (e.g. induced by the dopamine releaser amphetamine). Finally, selective antagonist PET radioligands for the dopamine D4 receptor have recently been synthesized and evaluated successfully in small laboratory animals, although these radioligands have not yet been reported as applied in human subjects. In conclusion, after almost four decades of research, several relevant parts of the central dopamine system can be assessed quantitatively in the living human brain using PET or SPECT. Future studies may include application of agonist radioligands and more dopamine receptor subtype selective radioligands.
UR - https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=85099967225&origin=inward
UR - https://www.ncbi.nlm.nih.gov/pubmed/37313129
U2 - https://doi.org/10.1007/978-3-030-53176-8_11
DO - https://doi.org/10.1007/978-3-030-53176-8_11
M3 - Chapter
SN - 9783030531751
T3 - PET and SPECT of Neurobiological Systems
SP - 295
EP - 318
BT - PET and SPECT of Neurobiological Systems
PB - Springer International Publishing
ER -