Synthesis of S-([18F]fluoromethyl)-(+)-McN5652 as a potential PET radioligand for the serotonin transporter

The present study describes the synthesis of the [18F]fluoromethyl analogue of (+)-McN5652 ([18F]FMe-McN) as a new potential tracer for the serotonin transporter. In vitro binding studies have shown that FMe-McN displays only slightly lower affinity for the serotonin transporter (K(i) = 2.3 +/- 0.1...

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Bibliographic Details
Published in:Nuclear medicine and biology 2001-10, Vol.28 (7), p.857-863
Main Authors: ZESSIN, Jörg, ESKOLA, Olli, BRUST, Peter, BERGMAN, Jörgen, STEINBACH, Jörg, LEHIKOINEN, Pertti, SOLIN, Olof, JOHANNSEN, Bernd
Format: Article
Language:English
Subjects:
Animals
Biological and medical sciences
Carrier Proteins - metabolism
Caudate Nucleus - metabolism
Contrast media. Radiopharmaceuticals
Drug Stability
Fluorine Radioisotopes
In Vitro Techniques
Indicators and Reagents
Investigative techniques, diagnostic techniques (general aspects)
Isoquinolines - chemical synthesis
Isotope Labeling
Magnetic Resonance Spectroscopy
Medical sciences
Membrane Glycoproteins - metabolism
Membrane Transport Proteins
Nerve Tissue Proteins
Nervous system
Paroxetine - metabolism
Pharmacology. Drug treatments
Radioligand Assay
Radionuclide investigations
Radiopharmaceuticals - chemical synthesis
Radiopharmaceuticals - pharmacology
Serotonin Antagonists - chemical synthesis
Serotonin Plasma Membrane Transport Proteins
Serotonin Uptake Inhibitors - metabolism
Solvents
Swine
Tomography, Emission-Computed
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Summary:The present study describes the synthesis of the [18F]fluoromethyl analogue of (+)-McN5652 ([18F]FMe-McN) as a new potential tracer for the serotonin transporter. In vitro binding studies have shown that FMe-McN displays only slightly lower affinity for the serotonin transporter (K(i) = 2.3 +/- 0.1 nM) than (+)-McN5652 (K(i) = 0.72 +/- 0.2 nM). The radiofluorinated tracer [18F]FMe-McN was prepared by reaction of normethyl (+)-McN5652 with the fluoromethylation agent [18F]bromofluoromethane in an overall radiochemical yield of 5 +/- 1% (decay-corrected, related to [18F]fluoride) and with high specific radioactivity (200-2,000 GBq/micromol at the end of synthesis).
ISSN:0969-8051
1872-9614
DOI:10.1016/S0969-8051(01)00248-7