Synthesis, Characterization, and Binding to the Translocator Protein (18 kDa, TSPO) of a New Rhenium Complex as a Model of Radiopharmaceutical Agents

2013 ◽  
Vol 639 (8-9) ◽  
pp. 1606-1612 ◽  
Author(s):  
Sara Piccinonna ◽  
Nunzio Denora ◽  
Nicola Margiotta ◽  
Valentino Laquintana ◽  
Giuseppe Trapani ◽  
...  
Keyword(s):  
Translocator Protein ◽  
Rhenium Complex ◽  
Translocator Protein 18 Kda ◽  
Radiopharmaceutical Agents

Structural and Functional Evolution of the Translocator Protein (18 kDa)

2012 ◽  
Vol 12 (4) ◽  
pp. 369-386 ◽  
Author(s):  
J. Fan ◽  
P. Lindemann ◽  
M. G.J. Feuilloley ◽  
V. Papadopoulos
Keyword(s):  
Translocator Protein ◽  
Functional Evolution ◽  
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.

scholarly journals Effects of Translocator Protein (18 kDa) Ligands on Microglial Activation and Neuronal Death in the Quinolinic-Acid-Injected Rat Striatum

2012 ◽  
Vol 3 (2) ◽  
pp. 114-119 ◽  
Author(s):  
Katherine R. Leaver ◽  
Aaron Reynolds ◽  
Sylvie Bodard ◽  
Denis Guilloteau ◽  
Sylvie Chalon ◽  
...  
Keyword(s):  
Quinolinic Acid ◽  
Neuronal Death ◽  
Microglial Activation ◽  
Translocator Protein ◽  
Rat Striatum ◽  
Translocator Protein 18 Kda

scholarly journals 6.1 STUDY OF ALTERED NEUROIMMUNITY IN PSYCHOSIS USING PET-BASED IMAGING OF THE TRANSLOCATOR PROTEIN 18 KDA: PROMISES, PITFALLS, AND FUTURE DIRECTIONS

2018 ◽  
Vol 44 (suppl_1) ◽  
pp. S8-S8
Author(s):  
Jennifer Coughlin ◽  
Tina Notter ◽  
Yong Du ◽  
Martin Pomper ◽  
Akira Sawa ◽  
...  
Keyword(s):  
Translocator Protein ◽  
Future Directions ◽  
Translocator Protein 18 Kda

Intracellular cholesterol changes induced by translocator protein (18 kDa) TSPO/PBR ligands

2007 ◽  
Vol 53 (2) ◽  
pp. 318-329 ◽  
Author(s):  
Angela Maria Falchi ◽  
Barbara Battetta ◽  
Francesca Sanna ◽  
Marco Piludu ◽  
Valeria Sogos ◽  
...  
Keyword(s):  
Translocator Protein ◽  
Translocator Protein 18 Kda ◽  
Intracellular Cholesterol
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