Effective MicroPET imaging of brain 5‐HT1A receptors in rats with [18F]MeFWAY by suppression of radioligand defluorination

@article{Choi2012EffectiveMI,
  title={Effective MicroPET imaging of brain 5‐HT1A receptors in rats with [18F]MeFWAY by suppression of radioligand defluorination},
  author={Jae Yong Choi and Chul Hoon Kim and Tae Joo Jeon and Byoung Soo Kim and Chi Hoon Yi and Kwang Sun Woo and Young Beom Seo and Sang Jin Han and KyeongMin Kim and Dae Ik Yi and Minkyung Lee and Dong Goo Kim and Jung Young Kim and Kyochul Lee and Tae-Hyun Choi and Gwang Il An and Young Hoon Ryu},
  journal={Synapse},
  year={2012},
  volume={66}
}
  • J. ChoiC. Kim Y. Ryu
  • Published 1 December 2012
  • Biology, Medicine, Chemistry
  • Synapse
Introduction: [18F]MeFWAY has been developed for imaging the serotonin 1A receptors in the brain. The purpose of this study were to verify the metabolic stability of [18F]MeFWAY, to measure the degree of defluorination of [18F]MeFWAY in vivo, to investigate methods of inhibition of defluorination of [18F]MeFWAY, and to assess the efficacy of [18F]MeFWAY in rat brains in vivo. Methods: MicroPET experiments in rats were conducted to confirm the distribution of radioactivity in the brain… 
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15 Citations
Background Citations
4
Methods Citations
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15 Citations

Translational possibility of [18F]Mefway to image serotonin 1A receptors in humans: Comparison with [18F]FCWAY in rodents

[18F]Mefway exhibits favorable characteristics compared to [18F]:FCWAY in rodents, and may be a promising radioligand for use in human subjects.

First-in-Human Evaluation of 18F-Mefway, a PET Radioligand Specific to Serotonin-1A Receptors

The simple radiosynthesis, high specific binding profile, and absence of PET signal in bone make 18F-mefway an attractive radiotracer for PET experiments examining the 5-HT1A receptor in neuropsychiatric disorders and drug intervention in humans.

18F-Mefway PET Imaging of Serotonin 1A Receptors in Humans: A Comparison with 18F-FCWAY

18F-Mefway may be a good candidate PET radioligand for 5-HT1A receptor imaging in human and the resistance to in vivo defluorination of 18F- Mefway obviates the need for the use of a defLuorination inhibitor.

Dopaminergic neuron destruction reduces hippocampal serotonin 1A receptor uptake of trans-[(18)F]Mefway.

  • Minkyung LeeY. Ryu J. Choi
  • Biology, Psychology
    Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine
  • 2014

Optimization of the radiosynthesis of [(18) F]MEFWAY for imaging brain serotonin 1A receptors by using the GE TracerLab FXFN-Pro module.

  • J. ChoiC. Kim T. Jeon
  • Chemistry
    Journal of labelled compounds & radiopharmaceuticals
  • 2013
The aim of this study was to develop a highly reliable radiofluorination method for the preparation of N-{2-[4-(2-methoxyphenyl)piperazinyl]ethyl}-N-(2-pyridyl)-N-(4-(18)…

P-Glycoprotein, not BCRP, Limits the Brain Uptake of [18F]Mefway in Rodent Brain

Mefway is modulated by P-gp, and not by Bcrp in rodents, as shown in Figure 18F.

Radiofluorinated N-Octanoyl Dopamine ([18F]F-NOD) as a Tool To Study Tissue Distribution and Elimination of NOD in Vitro and in Vivo.

In vitro, low cell association was found for [18F]5, indicating no active transport mechanism into cells, and data suggest that also NOD might be cleared fast, further pharmacokinetic evaluation is warranted.

Optimal timing of [¹⁸F]Mefway PET for imaging the serotonin 1A receptor in healthy male subjects.

Acute physical stress induces the alteration of the serotonin 1A receptor density in the hippocampus

The data illustrates that an acute physical stress induces the change in the serotonergic system that correlates with the behavioral despair.

Relationship between dopamine deficit and the expression of depressive behavior resulted from alteration of serotonin system

It is demonstrated that the destruction of dopaminergic system causes the reduction of the serotonergic system resulting in the expression of depressive behavior.

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