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18F-Mefway PET imaging of serotonin 1A receptors in humans: a comparison with 18F-FCWAY

 Jae Yong Choi  ;  Chul Hyoung Lyoo  ;  Jin Su Kim  ;  Kyeong Min Kim  ;  Jee Hae Kang  ;  Soo-Hee Choi  ;  Jae-Jin Kim  ;  Young Hoon Ryu 
 PLOS ONE, Vol.10(4) : e0121342, 2015 
Journal Title
Issue Date
Adult ; Area Under Curve ; Brain/diagnostic imaging ; Brain/metabolism ; Cyclohexanes/chemical synthesis ; Cyclohexanes/chemistry* ; Fluorine Radioisotopes/chemistry ; Humans ; Male ; Piperazines/chemical synthesis ; Piperazines/chemistry* ; Positron-Emission Tomography/methods* ; Pyridines/chemical synthesis ; Pyridines/chemistry* ; ROC Curve ; Radiopharmaceuticals/chemical synthesis ; Radiopharmaceuticals/chemistry* ; Receptor, Serotonin, 5-HT1A/metabolism ; Skull/diagnostic imaging ; Skull/metabolism ; Tomography, X-Ray Computed
INTRODUCTION: The purpose of this research is to evaluate the prospects for the use of 4-(trans-18F-fluoranylmethyl)-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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1. College of Medicine (의과대학) > Dept. of Neurology (신경과학교실) > 1. Journal Papers
1. College of Medicine (의과대학) > Dept. of Nuclear Medicine (핵의학교실) > 1. Journal Papers
1. College of Medicine (의과대학) > Dept. of Psychiatry (정신과학교실) > 1. Journal Papers
Yonsei Authors
Kim, Jae Jin(김재진) ORCID logo https://orcid.org/0000-0002-1395-4562
Lyoo, Chul Hyoung(류철형) ORCID logo https://orcid.org/0000-0003-2231-672X
Ryu, Young Hoon(유영훈) ORCID logo https://orcid.org/0000-0002-9000-5563
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