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KMID : 0043320120350091591
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Archives of Pharmacal Research
2012 Volume.35 No. 9 p.1591 ~ p.1597
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Compartmental modeling and simplified quantification of [11C]sertraline distribution in human brain
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Kim Ji-Who
Lee Jae-Sung
Kim Su-Jin
Hoigebazar Lathika
Shin Kwang-Hee
Yu Kyung-Sang
Ahn Won-Sik
Jeong Jae-Min
Lee Dong-Soo
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Abstract
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Sertraline hydrochloride (Zoloft®, Pfizer) is an antidepressant drug of the selective serotonin reuptake inhibitor (SSRI). The aims of this study were evaluating its in vivo distribution and kinetic models in human brain. Also, this study was to determine optimal scan duration of dynamic positron emission tomography (PET) for accurate [11C]sertraline kinetic parameters and the feasibility of semi-quantitative approach for assessing distribution volume ratio (DVR). [11C]sertraline dynamic PET and magnetic resonance imaging (MRI) scans were performed in 5 healthy males. Blood sampling were collected for the input function. Tissue time-activity curves (TAC) were obtained in 7 brain regions using MRI. Goodness-of-fit for TAC using simple tissue compartment model (2C2P) and 3-compartment models with irreversible (3C3P) and reversible (3C4P) were compared. Total distribution volume (DV) for each region of interest (ROI) and DVR were calculated. Also, ratio between the standard uptake value (SUV) of each ROI and that of cerebellum (SUVr) was computed and correlated with the DVR. Akaike information criteria analysis showed that the 2C2P was the most suitable model. Average values of K1 (mL/min/g) and k2 (1/min) were 0.54 and 0.012 in putamen. PET scan time longer than 50 min was required for the accurate estimation of DV. SUVr in 50?90 min was well correlated with DVR.
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KEYWORD
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Departments of Kinetic modeling, Serotonin transporters, Pharmacokinetics, PET, [11C]sertraline, Microdose
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