10.1002/jlcr.3206
https://zenodo.org/records/11267
oai:zenodo.org:11267
Janssen, Bieneke
Bieneke
Janssen
Department of Radiology and Nuclear Medicine, VU University Medical Center, Amsterdam, The Netherlands
Vugts, Danielle J
Danielle J
Vugts
Department of Radiology and Nuclear Medicine, VU University Medical Center, Amsterdam, The Netherlands
Funke, Uta
Uta
Funke
Department of Radiology and Nuclear Medicine, VU University Medical Center, Amsterdam, The Netherlands and BV Cyclotron VU, Amsterdam, The Netherlands
Spaans, Arnold
Arnold
Spaans
Department of Radiology and Nuclear Medicine, VU University Medical Center, Amsterdam, The Netherlands and BV Cyclotron VU, Amsterdam, The Netherlands
Schuit, Robert C
Robert C
Schuit
Department of Radiology and Nuclear Medicine, VU University Medical Center, Amsterdam, The Netherlands
Kooijman, Esther
Esther
Kooijman
Department of Radiology and Nuclear Medicine, VU University Medical Center, Amsterdam, The Netherlands
Rongen, Marissa
Marissa
Rongen
Department of Radiology and Nuclear Medicine, VU University Medical Center, Amsterdam, The Netherlands
Perk, Lars R
Lars R
Perk
BV Cyclotron VU, Amsterdam, The Netherlands
Lammertsma, Adriaan A
Adriaan A
Lammertsma
Department of Radiology and Nuclear Medicine, VU University Medical Center, Amsterdam, The Netherlands
Windhorst, Albert D
Albert D
Windhorst
Department of Radiology and Nuclear Medicine, VU University Medical Center, Amsterdam, The Netherlands
Synthesis and initial preclinical evaluation of the P2X7 receptor antagonist [11C]A-740003 as a novel tracer of neuroinflammation
Zenodo
2014
radiolabelling
carbon-11
A-740003
P2X7 receptor
neuroinflammation
positron emission tomography
2014-07-03
https://zenodo.org/communities/inmind
https://zenodo.org/communities/eu
Neuroinflammation, in particular activation of microglia, is thought to play an important role in the progression of
neurodegenerative diseases. In activated microglia, the purinergic P2X7 receptor is upregulated. A-740003, a highly affine
and selective P2X7 receptor antagonist, is a promising candidate for the development of a radiotracer for imaging of
neuroinflammation by positron emission tomography. For this purpose, [11C]A-740003 was synthesised and evaluated
in vivo with respect to both tracer metabolism and biodistribution. In plasma, a moderate metabolic rate was seen. In healthy rat brain, only marginal uptake of [11C]A-740003 was observed and, therefore, metabolites in brain could not be determined. Whether the minimal brain uptake is due to the low expression levels of the P2X7 receptor in healthy brain or to limited transport across the blood–brain barrier has yet to be elucidated.
European Commission
10.13039/501100000780
278850
Imaging of Neuroinflammation in Neurodegenerative Diseases