18F-Mefway PET imaging of serotonin 1A receptors in humans

A comparison with 18F-FCWAY

Jae Yong Choi, Chulhyoung Lyoo, Jin Su Kim, Kyeong Min Kim, Jee Hae Kang, Soo Hee Choi, Jae-Jin Kim, Young Hoon Ryu

Research output: Contribution to journalArticle

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Abstract

Introduction The purpose of this research is to evaluate the prospects for the use of 4-(trans-18F-fluora-nylmethyl)-N -[2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl]-N-pyridin-2-ylcyclohexane-1-carboxamide (18F-Mefway) in comparison to 18F-trans-4-fluoro-N-2-[4-(2-methoxyphenyl) piperazin-1-yl]ethyl]-N-(2-pyridyl)cyclohexanecarboxamide (18F-FCWAY) for the quantification of 5-HT1A receptors in human subjects. Method Five healthy male controls were included for two positron emission tomography (PET) studies: 18F-FCWAY PET after the pretreatment with 500 mg of disulfiram and two months later, 18F-Mefway PET without disulfiram. Regional time-activity curves (TACs) were extracted from nine cortical and subcortical regions in dynamic PET images. Using cerebellar cortex without vermis as reference tissue, in vivo kinetics for both radioligands were compared based on the distribution volume ratio (DVR) calculated by non-invasive Logan graphical analysis and area under the curve ratio of the TACs (AUC ratio). Result Although the pattern of regional uptakes in the 18F-Mefway PET was similar to that of the 18F-FCWAY PET (highest in the hippocampus and lowest in the cerebellar cortex), the amount of regional uptake in 18F-Mefway PET was almost half of that in 18F-FCWAY PET. The skull uptake in 18F-Mefway PET was only 25% of that in 18F-FCWAY PET with disulfiram pretreatment. The regional DVR values and AUC ratio values for 18F-Mefway were 17-40% lower than those of 18F-FCWAY. In contrast to a small overestimation of DVR values by AUC ratio values (< 10%) in 18F-FCWAY PET, the overestimation bias of AUC ratio values was much higher (up to 21%) in 18F-Mefway PET. Conclusion As 18F-Mefway showed lower DVR values and greater overestimation bias of AUC ratio values, 18F-Mefway may appear less favorable than 18F-FCWAY. However, in contrast to 18F-FCWAY, the resistance to in vivo defluorination of 18F-Mefway obviates the need for the use of a defluorination inhibitor. Thus, 18F-Mefway may be a good candidate PET radioligand for 5-HT1A receptor imaging in human.

Original languageEnglish
Article numbere0121342
JournalPLoS One
Volume10
Issue number4
DOIs
Publication statusPublished - 2015 Apr 1

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positron-emission tomography
Receptor, Serotonin, 5-HT1A
Positron emission tomography
serotonin
Positron-Emission Tomography
image analysis
Imaging techniques
receptors
disulfiram
Area Under Curve
Disulfiram
Cerebellar Cortex
N-(2-(4-(2-methoxyphenyl)piperazino))-N-(2-pyridinyl) trans-4-fluorocyclohexanecarboxamide
mefway
cortex
pretreatment
hippocampus
Skull
skull
Hippocampus

All Science Journal Classification (ASJC) codes

  • Biochemistry, Genetics and Molecular Biology(all)
  • Agricultural and Biological Sciences(all)

Cite this

Choi, J. Y., Lyoo, C., Kim, J. S., Kim, K. M., Kang, J. H., Choi, S. H., ... Ryu, Y. H. (2015). 18F-Mefway PET imaging of serotonin 1A receptors in humans: A comparison with 18F-FCWAY. PLoS One, 10(4), [e0121342]. https://doi.org/10.1371/journal.pone.0121342
Choi, Jae Yong ; Lyoo, Chulhyoung ; Kim, Jin Su ; Kim, Kyeong Min ; Kang, Jee Hae ; Choi, Soo Hee ; Kim, Jae-Jin ; Ryu, Young Hoon. / 18F-Mefway PET imaging of serotonin 1A receptors in humans : A comparison with 18F-FCWAY. In: PLoS One. 2015 ; Vol. 10, No. 4.
@article{e5cdb73d02164b1b8425b301257107e5,
title = "18F-Mefway PET imaging of serotonin 1A receptors in humans: A comparison with 18F-FCWAY",
abstract = "Introduction The purpose of this research is to evaluate the prospects for the use of 4-(trans-18F-fluora-nylmethyl)-N -[2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl]-N-pyridin-2-ylcyclohexane-1-carboxamide (18F-Mefway) in comparison to 18F-trans-4-fluoro-N-2-[4-(2-methoxyphenyl) piperazin-1-yl]ethyl]-N-(2-pyridyl)cyclohexanecarboxamide (18F-FCWAY) for the quantification of 5-HT1A receptors in human subjects. Method Five healthy male controls were included for two positron emission tomography (PET) studies: 18F-FCWAY PET after the pretreatment with 500 mg of disulfiram and two months later, 18F-Mefway PET without disulfiram. Regional time-activity curves (TACs) were extracted from nine cortical and subcortical regions in dynamic PET images. Using cerebellar cortex without vermis as reference tissue, in vivo kinetics for both radioligands were compared based on the distribution volume ratio (DVR) calculated by non-invasive Logan graphical analysis and area under the curve ratio of the TACs (AUC ratio). Result Although the pattern of regional uptakes in the 18F-Mefway PET was similar to that of the 18F-FCWAY PET (highest in the hippocampus and lowest in the cerebellar cortex), the amount of regional uptake in 18F-Mefway PET was almost half of that in 18F-FCWAY PET. The skull uptake in 18F-Mefway PET was only 25{\%} of that in 18F-FCWAY PET with disulfiram pretreatment. The regional DVR values and AUC ratio values for 18F-Mefway were 17-40{\%} lower than those of 18F-FCWAY. In contrast to a small overestimation of DVR values by AUC ratio values (< 10{\%}) in 18F-FCWAY PET, the overestimation bias of AUC ratio values was much higher (up to 21{\%}) in 18F-Mefway PET. Conclusion As 18F-Mefway showed lower DVR values and greater overestimation bias of AUC ratio values, 18F-Mefway may appear less favorable than 18F-FCWAY. However, in contrast to 18F-FCWAY, the resistance to in vivo defluorination of 18F-Mefway obviates the need for the use of a defluorination inhibitor. Thus, 18F-Mefway may be a good candidate PET radioligand for 5-HT1A receptor imaging in human.",
author = "Choi, {Jae Yong} and Chulhyoung Lyoo and Kim, {Jin Su} and Kim, {Kyeong Min} and Kang, {Jee Hae} and Choi, {Soo Hee} and Jae-Jin Kim and Ryu, {Young Hoon}",
year = "2015",
month = "4",
day = "1",
doi = "10.1371/journal.pone.0121342",
language = "English",
volume = "10",
journal = "PLoS One",
issn = "1932-6203",
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18F-Mefway PET imaging of serotonin 1A receptors in humans : A comparison with 18F-FCWAY. / Choi, Jae Yong; Lyoo, Chulhyoung; Kim, Jin Su; Kim, Kyeong Min; Kang, Jee Hae; Choi, Soo Hee; Kim, Jae-Jin; Ryu, Young Hoon.

In: PLoS One, Vol. 10, No. 4, e0121342, 01.04.2015.

Research output: Contribution to journalArticle

TY - JOUR

T1 - 18F-Mefway PET imaging of serotonin 1A receptors in humans

T2 - A comparison with 18F-FCWAY

AU - Choi, Jae Yong

AU - Lyoo, Chulhyoung

AU - Kim, Jin Su

AU - Kim, Kyeong Min

AU - Kang, Jee Hae

AU - Choi, Soo Hee

AU - Kim, Jae-Jin

AU - Ryu, Young Hoon

PY - 2015/4/1

Y1 - 2015/4/1

N2 - Introduction The purpose of this research is to evaluate the prospects for the use of 4-(trans-18F-fluora-nylmethyl)-N -[2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl]-N-pyridin-2-ylcyclohexane-1-carboxamide (18F-Mefway) in comparison to 18F-trans-4-fluoro-N-2-[4-(2-methoxyphenyl) piperazin-1-yl]ethyl]-N-(2-pyridyl)cyclohexanecarboxamide (18F-FCWAY) for the quantification of 5-HT1A receptors in human subjects. Method Five healthy male controls were included for two positron emission tomography (PET) studies: 18F-FCWAY PET after the pretreatment with 500 mg of disulfiram and two months later, 18F-Mefway PET without disulfiram. Regional time-activity curves (TACs) were extracted from nine cortical and subcortical regions in dynamic PET images. Using cerebellar cortex without vermis as reference tissue, in vivo kinetics for both radioligands were compared based on the distribution volume ratio (DVR) calculated by non-invasive Logan graphical analysis and area under the curve ratio of the TACs (AUC ratio). Result Although the pattern of regional uptakes in the 18F-Mefway PET was similar to that of the 18F-FCWAY PET (highest in the hippocampus and lowest in the cerebellar cortex), the amount of regional uptake in 18F-Mefway PET was almost half of that in 18F-FCWAY PET. The skull uptake in 18F-Mefway PET was only 25% of that in 18F-FCWAY PET with disulfiram pretreatment. The regional DVR values and AUC ratio values for 18F-Mefway were 17-40% lower than those of 18F-FCWAY. In contrast to a small overestimation of DVR values by AUC ratio values (< 10%) in 18F-FCWAY PET, the overestimation bias of AUC ratio values was much higher (up to 21%) in 18F-Mefway PET. Conclusion As 18F-Mefway showed lower DVR values and greater overestimation bias of AUC ratio values, 18F-Mefway may appear less favorable than 18F-FCWAY. However, in contrast to 18F-FCWAY, the resistance to in vivo defluorination of 18F-Mefway obviates the need for the use of a defluorination inhibitor. Thus, 18F-Mefway may be a good candidate PET radioligand for 5-HT1A receptor imaging in human.

AB - Introduction The purpose of this research is to evaluate the prospects for the use of 4-(trans-18F-fluora-nylmethyl)-N -[2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl]-N-pyridin-2-ylcyclohexane-1-carboxamide (18F-Mefway) in comparison to 18F-trans-4-fluoro-N-2-[4-(2-methoxyphenyl) piperazin-1-yl]ethyl]-N-(2-pyridyl)cyclohexanecarboxamide (18F-FCWAY) for the quantification of 5-HT1A receptors in human subjects. Method Five healthy male controls were included for two positron emission tomography (PET) studies: 18F-FCWAY PET after the pretreatment with 500 mg of disulfiram and two months later, 18F-Mefway PET without disulfiram. Regional time-activity curves (TACs) were extracted from nine cortical and subcortical regions in dynamic PET images. Using cerebellar cortex without vermis as reference tissue, in vivo kinetics for both radioligands were compared based on the distribution volume ratio (DVR) calculated by non-invasive Logan graphical analysis and area under the curve ratio of the TACs (AUC ratio). Result Although the pattern of regional uptakes in the 18F-Mefway PET was similar to that of the 18F-FCWAY PET (highest in the hippocampus and lowest in the cerebellar cortex), the amount of regional uptake in 18F-Mefway PET was almost half of that in 18F-FCWAY PET. The skull uptake in 18F-Mefway PET was only 25% of that in 18F-FCWAY PET with disulfiram pretreatment. The regional DVR values and AUC ratio values for 18F-Mefway were 17-40% lower than those of 18F-FCWAY. In contrast to a small overestimation of DVR values by AUC ratio values (< 10%) in 18F-FCWAY PET, the overestimation bias of AUC ratio values was much higher (up to 21%) in 18F-Mefway PET. Conclusion As 18F-Mefway showed lower DVR values and greater overestimation bias of AUC ratio values, 18F-Mefway may appear less favorable than 18F-FCWAY. However, in contrast to 18F-FCWAY, the resistance to in vivo defluorination of 18F-Mefway obviates the need for the use of a defluorination inhibitor. Thus, 18F-Mefway may be a good candidate PET radioligand for 5-HT1A receptor imaging in human.

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DO - 10.1371/journal.pone.0121342

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