PMID- 22136885
OWN - NLM
STAT- MEDLINE
DCOM- 20120629
LR  - 20221207
IS  - 1872-9614 (Electronic)
IS  - 0969-8051 (Linking)
VI  - 39
IP  - 2
DP  - 2012 Feb
TI  - Characterization of 4-[18F]-ADAM as an imaging agent for SERT in non-human 
      primate brain using PET: a dynamic study.
PG  - 279-85
LID - 10.1016/j.nucmedbio.2011.08.002 [doi]
AB  - INTRODUCTION: Serotonin transporter (SERT) has been associated with many 
      psychiatric diseases. This study investigated the biodistribution of a serotonin 
      transporter imaging agent, 
      N,N-dimethyl-2-(2-amino-4-(18)F-fluorophenylthio)benzylamine (4-[(18)F]-ADAM), in 
      nonhuman primate brain using positron emission tomography (PET). METHODS: Six and 
      four Macaca cyclopis monkeys were used to determine the transit time (i.e., time 
      necessary to reach biodistribution equilibrium) and the reproducibility of 
      4-[(18)F]-ADAM biodistribution in the brain, respectively. The sensitivity and 
      specificity of 4-[(18)F]-ADAM binding to SERT were evaluated in one monkey 
      challenged with different doses of fluoxetine and one monkey treated with 
      3,4-methylendioxymethamphetamine (MDMA). Dynamic PET imaging was performed for 3 
      h after 4-[(18)F]-ADAM intravenous bolus injection. The specific uptake ratios 
      (SURs) in the midbrain (MB), thalamus (TH), striatum (ST) and frontal cortex (FC) 
      were calculated. RESULTS: The distribution of 4-[(18)F]-ADAM reached equilibrium 
      120-150 min after injection. The mean SURs were 2.49 +/- 0.13 in MB, 1.59 +/- 0.17 in 
      TH, 1.35 +/- 0.06 in ST and 0.34 +/- 0.03 in FC, and the minimum variability was 
      shown 120-150 min after 4-[(18)F]-ADAM injection. Using SURs and intraclass 
      coefficient of correlation, the test/retest variability was under 8% and above 
      0.8, respectively, in SERT-rich areas. Challenge with fluoxetin (0.75-2 mg) 
      dose-dependently inhibited the SURs in various brain regions. 4-[(18)F]-ADAM 
      binding was markedly reduced in the brain of an MDMA-treated monkey compared to 
      that in brains of normal controls. CONCLUSION: 4-[(18)F]-ADAM appears to be a 
      highly selective radioligand for imaging SERT in monkey brain.
CI  - Copyright (c) 2012 Elsevier Inc. All rights reserved.
FAU - Chen, Yu-An
AU  - Chen YA
AD  - Graduate Institute of Life Sciences, National Defense Medical Center, 114 Taipei, 
      Taiwan.
FAU - Huang, Wen-Sheng
AU  - Huang WS
FAU - Lin, Yaoh-Shiang
AU  - Lin YS
FAU - Cheng, Cheng-Yi
AU  - Cheng CY
FAU - Liu, Ren-Shyan
AU  - Liu RS
FAU - Wang, Shyh-Jen
AU  - Wang SJ
FAU - Li, I-Hsun
AU  - Li IH
FAU - Huang, San-Yuan
AU  - Huang SY
FAU - Shiue, Chyng-Yann
AU  - Shiue CY
FAU - Chen, Cheng-Yu
AU  - Chen CY
FAU - Ma, Kuo-Hsing
AU  - Ma KH
LA  - eng
PT  - Journal Article
DEP - 20111201
PL  - United States
TA  - Nucl Med Biol
JT  - Nuclear medicine and biology
JID - 9304420
RN  - 0 (Benzylamines)
RN  - 0 (Fluorine Radioisotopes)
RN  - 0 (N,N-dimethyl-2-(2-amino-4-fluorophenylthio)benzylamine)
RN  - 0 (Serotonin Agents)
RN  - 0 (Serotonin Plasma Membrane Transport Proteins)
RN  - 0 (Serotonin Uptake Inhibitors)
RN  - 01K63SUP8D (Fluoxetine)
RN  - KE1SEN21RM (N-Methyl-3,4-methylenedioxyamphetamine)
SB  - IM
MH  - Animals
MH  - Benzylamines/*pharmacokinetics
MH  - Brain/*diagnostic imaging/metabolism
MH  - Female
MH  - Fluorine Radioisotopes/*pharmacokinetics
MH  - Fluoxetine/pharmacology
MH  - Macaca
MH  - Male
MH  - N-Methyl-3,4-methylenedioxyamphetamine/pharmacology
MH  - Positron-Emission Tomography/*methods
MH  - Reproducibility of Results
MH  - Sensitivity and Specificity
MH  - Serotonin Agents/pharmacology
MH  - Serotonin Plasma Membrane Transport Proteins/*metabolism
MH  - Selective Serotonin Reuptake Inhibitors/pharmacology
MH  - Tissue Distribution
EDAT- 2011/12/06 06:00
MHDA- 2012/06/30 06:00
CRDT- 2011/12/06 06:00
PHST- 2011/05/26 00:00 [received]
PHST- 2011/07/21 00:00 [revised]
PHST- 2011/08/01 00:00 [accepted]
PHST- 2011/12/06 06:00 [entrez]
PHST- 2011/12/06 06:00 [pubmed]
PHST- 2012/06/30 06:00 [medline]
AID - S0969-8051(11)00188-0 [pii]
AID - 10.1016/j.nucmedbio.2011.08.002 [doi]
PST - ppublish
SO  - Nucl Med Biol. 2012 Feb;39(2):279-85. doi: 10.1016/j.nucmedbio.2011.08.002. Epub 
      2011 Dec 1.