scholarly journals Propofol Decreases In Vivo Binding of 11C-PBR28 to Translocator Protein (18 kDa) in the Human Brain

2012 ◽  
Vol 54 (1) ◽  
pp. 64-69 ◽  
Author(s):  
C. S. Hines ◽  
M. Fujita ◽  
S. S. Zoghbi ◽  
J. S. Kim ◽  
Z. Quezado ◽  
...  
Keyword(s):  
Human Brain ◽  
Translocator Protein ◽  
In Vivo Binding ◽  
Translocator Protein 18 Kda

scholarly journals Optimised GMP-compliant production of [18F]DPA-714 on the Trasis AllinOne module

2021 ◽  
Vol 6 (1) ◽  
Author(s):  
Klaudia A. Cybulska ◽  
Vera Bloemers ◽  
Lars R. Perk ◽  
Peter Laverman
Keyword(s):  
Significant Degree ◽  
Translocator Protein ◽  
Positron Emission ◽  
Leaving Group ◽  
Inflammatory Processes ◽  
Single Production ◽  
Translocator Protein 18 Kda ◽  
Radiochemical Yields ◽  
Specific Ligand

Abstract Background The translocator protein 18 kDa is recognised as an important biomarker for neuroinflammation due to its soaring expression in microglia. This process is common for various neurological disorders. DPA-714 is a potent TSPO-specific ligand which found its use in Positron Emission Tomography following substitution of fluorine-19 with fluorine-18, a positron-emitting radionuclide. [18F]DPA-714 enables visualisation of inflammatory processes in vivo non-invasively. Radiolabelling of this tracer is well described in literature, including validation for clinical use. Here, we report significant enhancements to the process which resulted in the design of a fully GMP-compliant robust synthesis of [18F]DPA-714 on a popular cassette-based system, Trasis AllinOne, boosting reliability, throughput, and introducing a significant degree of simplicity. Results [18F]DPA-714 was synthesised using the classic nucleophilic aliphatic substitution on a good leaving group, tosylate, with [18F]fluoride using tetraethylammonium bicarbonate in acetonitrile at 100∘C. The process was fully automated on a Trasis AllinOne synthesiser using an in-house designed cassette and sequence. With a relatively small precursor load of 4 mg, [18F]DPA-714 was obtained with consistently high radiochemical yields of 55-71% (n=6) and molar activities of 117-350 GBq/µmol at end of synthesis. With a single production batch, starting with 31-42 GBq of [18F]fluoride, between 13-20 GBq of the tracer can be produced, enabling multi-centre studies. Conclusion To the best of our knowledge, the process presented herein is the most efficient [18F]DPA-714 synthesis, with advantageous GMP compliance. The use of a Trasis AllinOne synthesiser increases reliability and allows rapid training of production staff.

In vitro and in vivo binding of dopamine D2-receptors with 123I iodobenzamide in rat and human brain

1990 ◽  
Vol 183 (4) ◽  
pp. 1414
Author(s):  
N.P.L.G. Verhoeff ◽  
M. Bobeldijk ◽  
E.A. van Royen ◽  
M.G.P. Feenstra ◽  
G.J. Boer ◽  
...  
Keyword(s):  
Human Brain ◽  
D2 Receptors ◽  
Dopamine D2 Receptors ◽  
In Vivo Binding ◽  
Dopamine D2

scholarly journals In vivo binding of protoporphyrin IX to rat translocator protein imaged with positron emission tomography

Synapse ◽  
2010 ◽  
Vol 64 (8) ◽  
pp. 649-653 ◽  
Author(s):  
Harushige Ozaki ◽  
Sami S. Zoghbi ◽  
Jinsoo Hong ◽  
Ajay Verma ◽  
Victor W. Pike ◽  
...  
Keyword(s):  
Positron Emission Tomography ◽  
Protoporphyrin Ix ◽  
Translocator Protein ◽  
Emission Tomography ◽  
In Vivo Binding ◽  
Positron Emission

scholarly journals Novel Pyrazolo[1,5-a]pyrimidines as Translocator Protein 18 kDa (TSPO) Ligands: Synthesis, in Vitro Biological Evaluation, [18F]-Labeling, and in Vivo Neuroinflammation PET Images

2015 ◽  
Vol 58 (18) ◽  
pp. 7449-7464 ◽  
Author(s):  
Annelaure Damont ◽  
Vincent Médran-Navarrete ◽  
Fanny Cacheux ◽  
Bertrand Kuhnast ◽  
Géraldine Pottier ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Translocator Protein ◽  
Translocator Protein 18 Kda

scholarly journals Quantification of Translocator Protein (18 kDa) in the Human Brain with PET and a Novel Radioligand, 18F-PBR06

2009 ◽  
Vol 50 (7) ◽  
pp. 1047-1053 ◽  
Author(s):  
Y. Fujimura ◽  
S. S. Zoghbi ◽  
F. G. Simeon ◽  
A. Taku ◽  
V. W. Pike ◽  
...  
Keyword(s):  
Human Brain ◽  
Translocator Protein ◽  
Translocator Protein 18 Kda

scholarly journals Voxel-Based Imaging of Translocator Protein 18Kda (TSPO) in High-Resolution PET

2013 ◽  
Vol 33 (3) ◽  
pp. 348-350 ◽  
Author(s):  
Ji Hyun Ko ◽  
Yuko Koshimori ◽  
Romina Mizrahi ◽  
Pablo Rusjan ◽  
Alan A Wilson ◽  
...  
Keyword(s):  
Relative Equilibrium ◽  
Compartment Model ◽  
Graphical Analysis ◽  
Translocator Protein ◽  
Proof Of Concept ◽  
Tissue Compartment ◽  
Potential Biomarker ◽  
Translocator Protein 18 Kda ◽  
Significant Attention

In vivo imaging of translocator protein 18 kDa (TSPO) has received significant attention as potential biomarker of microglia activation. Several radioligands have been designed with improved properties. Our group recently developed an 18F-labeled TSPO ligand, [18F]-FEPPA, and confirmed its reliability with a 2-tissue compartment model. Here, we extended, in a group of healthy subjects, its suitability for use in voxel-based analysis with the newly proposed graphical analysis approach, Relative-Equilibrium-Gjedde-Patlak (REGP) plot. The REGP plot successfully replicated the total distribution volumes estimated by the 2-tissue compartment model. We also showed its proof-of-concept in a patient with possible meningioma showing increased [18F]-FEPPA total distribution volume.

In vivo imaging of neuroinflammation in the rodent brain with [11C]SSR180575, a novel indoleacetamide radioligand of the translocator protein (18 kDa)

2010 ◽  
Vol 38 (3) ◽  
pp. 509-514 ◽  
Author(s):  
Fabien Chauveau ◽  
Hervé Boutin ◽  
Nadja Van Camp ◽  
Cyrille Thominiaux ◽  
Philippe Hantraye ◽  
...  
Keyword(s):  
In Vivo Imaging ◽  
Translocator Protein ◽  
Rodent Brain ◽  
Translocator Protein 18 Kda

Unbinding of Translocator Protein 18 kDa (TSPO) Ligands: From in Vitro Residence Time to in Vivo Efficacy via in Silico Simulations

2019 ◽  
Vol 10 (8) ◽  
pp. 3805-3814 ◽  
Author(s):  
Agostino Bruno ◽  
Elisabetta Barresi ◽  
Nicola Simola ◽  
Eleonora Da Pozzo ◽  
Barbara Costa ◽  
...  
Keyword(s):  
Residence Time ◽  
In Silico ◽  
Translocator Protein ◽  
In Vivo Efficacy ◽  
Translocator Protein 18 Kda

scholarly journals In vivo Evaluation of Inflammatory Bowel Disease with the Aid of μPET and the Translocator Protein 18 kDa Radioligand [18F]DPA-714

2014 ◽  
Vol 17 (1) ◽  
pp. 67-75 ◽  
Author(s):  
Nicholas Bernards ◽  
Géraldine Pottier ◽  
Benoit Thézé ◽  
Frédéric Dollé ◽  
Raphael Boisgard
Keyword(s):  
Inflammatory Bowel Disease ◽  
Bowel Disease ◽  
Translocator Protein ◽  
In Vivo Evaluation ◽  
Inflammatory Bowel ◽  
Translocator Protein 18 Kda

scholarly journals Translocator Protein (18 kDa) Polymorphism (rs6971) Explains in-vivo Brain Binding Affinity of the PET Radioligand [18F]-FEPPA

2012 ◽  
Vol 32 (6) ◽  
pp. 968-972 ◽  
Author(s):  
Romina Mizrahi ◽  
Pablo M Rusjan ◽  
James Kennedy ◽  
Bruce Pollock ◽  
Benoit Mulsant ◽  
...  
Keyword(s):  
Binding Affinity ◽  
Microglial Activation ◽  
Translocator Protein ◽  
Time Activity ◽  
Genetic Groups ◽  
Positron Emission ◽  
Translocator Protein 18 Kda ◽  
Human Brains ◽  
New Generation

[18F]-FEPPA binds to the 18-kDa translocator protein (TSPO) and is used in positron emission tomography (PET) to detect microglial activation. However, quantitative interpretations of the PET signal with new generation TSPO PET radioligands are confounded by large interindividual variability in binding affinity. This presents as a trimodal distribution, reflecting high-affinity binders (HABs), low-affinity binder (LAB), and mixed-affinity binders (MABs). Here, we show that one polymorphism (rs6971) located in exon 4 of the TSPO gene, which results in a nonconservative amino-acid substitution from alanine to threonine (Ala147Thr) in the TSPO protein, predicts [18F]-FEPPA total distribution volume in human brains. In addition, [18F]-FEPPA exhibits clearly different features in the shape of the time activity curves between genetic groups. Testing for the rs6971 polymorphism may allow quantitative interpretation of TSPO PET studies with new generation of TSPO PET radioligands.

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