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[11C]SMe-ADAM, an imaging agent for the brain serotonin transporter: synthesis, pharmacological characterization and microPET studies in rats.
- Source :
-
Nuclear medicine and biology [Nucl Med Biol] 2006 Jan; Vol. 33 (1), pp. 53-63. - Publication Year :
- 2006
-
Abstract
- N,N-Dimethyl-2-(2-amino-4-methylthiophenylthio)benzylamine (SMe-ADAM, 1) is a highly potent and selective inhibitor of the serotonin transporter (SERT). This compound was labeled with carbon-11 by methylation of the S-desmethyl precursor 10 with [(11)C]methyl iodide to obtain the potential positron emission tomography (PET) radioligand [(11)C]SMe-ADAM. The radiochemical yield was 27 +/- 5%, and the specific radioactivity was 26-40 GBq/micromol at the end of synthesis. Ex vivo and in vivo biodistribution experiments in rats demonstrated a rapid accumulation of the radiotracer in brain regions known to be rich in SERT, such as the thalamus/hypothalamus region (3.59 +/- 0.41%ID/g at 5 min after injection). The specific uptake reached a thalamus to cerebellum ratio of 6.74 +/- 0.95 at 60 min postinjection. The [(11)C]SMe-ADAM uptake in the thalamus was significantly decreased by pretreatment with fluoxetine to 38 +/- 11% of the control value. Furthermore, no metabolites of [(11)C]SMe-ADAM could be detected in the SERT-rich regions of the rat brain. It is concluded that [(11)C]SMe-ADAM may be a suitable PET ligand for SERT imaging in the living brain.
- Subjects :
- Animals
Carbon Radioisotopes
Male
Metabolic Clearance Rate
Organ Specificity
Positron-Emission Tomography veterinary
Radiopharmaceuticals pharmacokinetics
Rats
Rats, Sprague-Dawley
Reproducibility of Results
Tissue Distribution
Aniline Compounds pharmacokinetics
Brain diagnostic imaging
Brain metabolism
Positron-Emission Tomography methods
Serotonin Plasma Membrane Transport Proteins metabolism
Sulfides pharmacokinetics
Subjects
Details
- Language :
- English
- ISSN :
- 0969-8051
- Volume :
- 33
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Nuclear medicine and biology
- Publication Type :
- Academic Journal
- Accession number :
- 16459259
- Full Text :
- https://doi.org/10.1016/j.nucmedbio.2005.07.009