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

@article{Choi2014TranslationalPO,
  title={Translational possibility of [18F]Mefway to image serotonin 1A receptors in humans: Comparison with [18F]FCWAY in rodents},
  author={Jae Yong Choi and Byoung Soo Kim and Chul Hoon Kim and Dong Goo Kim and Sang Jin Han and Kyochul Lee and Kyeong‐Min Kim and Gwang Il An and Tae-Hyun Choi and Sun Dong Yoo and Young Hoon Ryu},
  journal={Synapse},
  year={2014},
  volume={68}
}
  • J. ChoiByoung Soo Kim Y. Ryu
  • Published 1 December 2014
  • Biology, Chemistry
  • Synapse
Purpose: To compare the cerebral uptake and binding potential of [18F]FCWAY and [18F]Mefway in the rodent to assess their potential for imaging serotonin 1A (5‐HT1A) receptors. Materials and Methods: In vitro liver microsomal studies were performed to evaluate the degree of defluorination. Dynamic positron emission tomography (PET) studies were then conducted for 2 h with or without an anti‐defluorination agent. The regions of interest were the hippocampus and frontal cortex (5‐HT1A target… 

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.

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.

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

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