Comparative evaluation of positron emission tomography radiotracers for imaging the norepinephrine transporter: (S,S) and (R,R) enantiomers of reboxetine analogs ([11C]methylreboxetine, 3‐Cl‐[11C]methylreboxetine and [18F]fluororeboxetine), (R)‐[11C]nisoxetine, [11C]oxaprotiline and [11C]lortalamine

@article{Ding2005ComparativeEO,
  title={Comparative evaluation of positron emission tomography radiotracers for imaging the norepinephrine transporter: (S,S) and (R,R) enantiomers of reboxetine analogs ([11C]methylreboxetine, 3‐Cl‐[11C]methylreboxetine and [18F]fluororeboxetine), (R)‐[11C]nisoxetine, [11C]oxaprotiline and [11C]lortalamine},
  author={Yu-Shin Ding and Kuo-Shyan Lin and Jean Logan and H{\'e}l{\`e}ne Benveniste and Pauline Carter},
  journal={Journal of Neurochemistry},
  year={2005},
  volume={94}
}
We have synthesized and evaluated several new ligands for imaging the norepinephrine transporter (NET) system in baboons with positron emission tomography (PET). Ligands possessing high brain penetration, high affinity and selectivity, appropriate lipophilicity (log P = 1.0–3.5), high plasma free fraction and reasonable stability in plasma were selected for further studies. Based on our characterization studies in baboons, including 11C‐labeled (R)‐nisoxetine (Nis), oxaprotiline (Oxap… 
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Synthesis of 11C-labelled (R)-OHDMI and CFMME and their evaluation as candidate radioligands for imaging central norepinephrine transporters with PET.
Imaging the norepinephrine transporter in humans with (S,S)-[11C]O-methyl reboxetine and PET: problems and progress.
Synthesis and PET evaluation of (R)‐[S‐methyl‐11C]thionisoxetine, a candidate radioligand for imaging brain norepinephrine transporters
TLDR
MPPP is an effective precursor for 11C-methylation to [11C]1, suggesting that the S-γ-propionic acid methyl ester protecting group may have wider value in the 12C-labeling of aryl methyl sulfides.
Evaluation of [11C]MRB for assessment of occupancy of norepinephrine transporters: Studies with atomoxetine in non-human primates
Synthesis, in vitro characterization, and radiolabeling of reboxetine analogs as potential PET radioligands for imaging the norepinephrine transporter.
18F-labeled norepinephrine transporter tracer [18F]NS12137: radiosynthesis and preclinical evaluation.
PET imaging of the effects of age and cocaine on the norepinephrine transporter in the human brain using (S,S)‐[11C]O‐methylreboxetine and HRRT
TLDR
It is suggested that brain NET concentration declines with age in HC, and there is a significant upregulation of NET in thalamus and dorsomedial thalamic nucleus in COC as compared to HC.
In vivo assessment of [11C]MRB as a prospective PET ligand for imaging the norepinephrine transporter
TLDR
Despite improvement over previous ligands for imaging NET in vivo, the low signal to noise ratio indicates [11C]MRB lacks sensitivity and reliability as a PET radiotracer in humans.
Preclinical Evaluation of the First Adenosine A1 Receptor Partial Agonist Radioligand for Positron Emission Tomography Imaging.
Central adenosine A1 receptor (A1R) is implicated in pain, sleep, substance use disorders, and neurodegenerative diseases, and is an important target for pharmaceutical development. Radiotracers for…
Identification and in vivo evaluation of a fluorine-18 rolipram analogue, [(18) F]MNI-617, as a radioligand for PDE4 imaging in mammalian brain.
TLDR
A small series of rolipram analogs that contain fluoro- or iodo-substituents that could be used as fluorine-18 PET or iodine-123 SPECT PDE4 radiotracers are described and evaluated in non-human primate, where it rapidly entered the brain, with SUVs between 4 and 5, and with a distribution pattern consistent with that of PDE 4.
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