Single-Step High-Yield Radiosynthesis and Evaluation of a Sensitive 18F-Labeled Ligand for Imaging Brain Peripheral Benzodiazepine Receptors with PET

E Briard, SS Zoghbi, FG Siméon… - Journal of medicinal …, 2009 - ACS Publications
Elevated levels of peripheral benzodiazepine receptors (PBR) are associated with activated
microglia in their response to inflammation. Hence, PBR imaging in vivo is valuable for …

Synthesis and Simple 18F-Labeling of 3-Fluoro-5-(2-(2-(fluoromethyl)thiazol-4-yl)ethynyl)benzonitrile as a High Affinity Radioligand for Imaging Monkey Brain …

FG Siméon, AK Brown, SS Zoghbi… - Journal of medicinal …, 2007 - ACS Publications
2-Fluoromethyl analogs of (3-[(2-methyl-1,3-thiazol-4yl)ethynyl]pyridine) were synthesized as
potential ligands for metabotropic glutamate subtype-5 receptors (mGluR5s). One of these, …

Synthesis and Screening in Mice of Fluorine-Containing PET Radioligands for TSPO: Discovery of a Promising 18F-Labeled Ligand

FG Siméon, JH Lee, CL Morse, I Stukes… - Journal of medicinal …, 2021 - ACS Publications
Translocator protein 18 kDa (TSPO) is a biomarker of neuroinflammation. [ 11 C]ER176
robustly quantifies TSPO in the human brain with positron emission tomography (PET), …

Syntheses of mGluR5 PET radioligands through the radiofluorination of diaryliodonium tosylates

S Telu, JH Chun, FG Siméon, S Lu… - Organic & biomolecular …, 2011 - pubs.rsc.org
3-Fluoro-1-((thiazol-4-yl)ethynyl)benzenes constitute an important class of high-affinity
metabotropic glutamate subtype 5 receptor (mGluR5) ligands, some of which have been labeled …

Metabotropic glutamate subtype 5 receptors are quantified in the human brain with a novel radioligand for PET

…, Y Kimura, SS Zoghbi, FG Siméon… - Journal of Nuclear …, 2008 - Soc Nuclear Med
We developed a radioligand, 3-fluoro-5-(2-(2- 18 F-(fluoromethyl)thiazol-4-yl)ethynyl)benzonitrile
( 18 F-SP203), for metabotropic glutamate subtype 5 (mGluR5) receptors that showed …

Radiodefluorination of 3-fluoro-5-(2-(2-[18F](fluoromethyl)-thiazol-4-yl) ethynyl) benzonitrile ([18F] SP203), a radioligand for imaging brain metabotropic glutamate …

HU Shetty, SS Zoghbi, FG Siméon, JS Liow… - … of Pharmacology and …, 2008 - ASPET
Metabotropic glutamate subtype-5 receptors (mGluR5) are implicated in several neuropsychiatric
disorders. Positron emission tomography (PET) with a suitable radioligand may enable …

Quantification of translocator protein (18 kDa) in the human brain with PET and a novel radioligand, 18F-PBR06

Y Fujimura, SS Zoghbi, FG Simeon… - Journal of Nuclear …, 2009 - Soc Nuclear Med
Translocator protein (TSPO) (18 kDa), formerly called the peripheral benzodiazepine
receptor, is upregulated on activated microglia and macrophages and is, thus, a biomarker of …

Biodistribution and radiation dosimetry in humans of a new PET ligand, 18F-PBR06, to image translocator protein (18 kDa)

Y Fujimura, Y Kimura, FG Siméon… - Journal of Nuclear …, 2010 - Soc Nuclear Med
As a PET biomarker for inflammation, translocator protein (18 kDa) (TSPO) can be
measured with an 18 F-labeled aryloxyanilide, 18 F-N-fluoroacetyl-N-(2,5-dimethoxybenzyl)-2-…

[HTML][HTML] Essential principles and recent progress in the development of TSPO PET ligands for neuroinflammation imaging

M Viviano, E Barresi, FG Siméon, B Costa… - Current medicinal …, 2022 - ncbi.nlm.nih.gov
The translocator protein 18kDa (TSPO) is expressed in the outer mitochondrial membrane
and is implicated in several functions, including cholesterol transport and steroidogenesis. …

[PDF][PDF] Integration of a microwave reactor with Synthia to provide a fully automated radiofluorination module

N Lazarova, FG Siméon, JL Musachio, S Lu… - Journal of Labelled …, 2007 - Citeseer
Microwave technology has been very successfully applied to enhance PET radiolabeling
reactions, including one-step nucleophilic radiofluorination reactions with [18F] fluoride ion, so …