PET imaging of the brain serotonin transporters (SERT) with N,N-dimethyl-2-(2-amino-4-[18F]fluorophenylthio)benzylamine (4-[ 18F]-ADAM) in humans: A preliminary study
Journal
European Journal of Nuclear Medicine and Molecular Imaging
Journal Volume
40
Journal Issue
1
Pages
115-124
Date Issued
2013
Author(s)
YA-YAO HUANG
Abstract
Purpose: The aim of this study was to assess the feasibility of using 4-[18F]-ADAM as a brain SERT imaging agent in humans. Methods: Enrolled in the study were 19 healthy Taiwanese subjects (11 men, 8 women; age 33 ± 9 years). The PET data were semiquantitatively analyzed and expressed as specific uptake ratios (SUR) and distribution volume ratios (DVR) using the software package PMOD. The SUR and DVR of 4-[18F]-ADAM in the raphe nucleus (RN), midbrain (MB), thalamus (TH), striatum (STR) and prefrontal cortex (PFC) were determined using the cerebellum (CB) as the reference region. Results: 4-[18F]-ADAM bound to known SERT-rich regions in human brain. The order of the regional brain uptake was MB (RN) > TH > STR > PFC > CB. The DVR (n = 4, t*= 60 min) in the RN, TH, STR and PFC were 3.00 ± 0.50, 2.25 ± 0.45, 2.05 ± 0.31 and 1.40 ± 0.13, respectively. The optimal time for imaging brain SERT with 4-[18F]-ADAM was 120-140 min after injection. At the optimal imaging time, the SURs (n = 15) in the MB, TH, STR, and PFC were 2.25 ± 0.20, 2.28 ± 0.20, 2.12 ± 0.18 and 1.47 ± 0.14, respectively. There were no significant differences in SERT availability between men and women (p < 0.05). Conclusion: The results of this study showed that 4-[ 18F]-ADAM was safe for human studies and its distribution in human brain appeared to correlate well with the known distribution of SERT in the human brain. In addition, it had high specific binding and a reasonable optimal time for imaging brain SERT in humans. Thus, 4-[18F]-ADAM may be feasible for assessing the status of brain SERT in humans. ? 2012 Springer-Verlag.
Subjects
4-[18F]-ADAM; Gender effects; Human study; PET; Serotonin transporters
SDGs
Other Subjects
n,n dimethyl 2 (2 amino 4 fluorophenylthio)benzylamine f 18; radiopharmaceutical agent; serotonin transporter; unclassified drug; adult; article; cerebellum; cerebellum cortex; clinical article; corpus striatum; drug distribution; drug uptake; female; human; image analysis; male; mesencephalon; positron emission tomography; prefrontal cortex; raphe nucleus; thalamus; Adult; Benzylamines; Brain; Female; Humans; Male; Positron-Emission Tomography; Radiopharmaceuticals; Serotonin Plasma Membrane Transport Proteins; Tissue Distribution
Type
journal article