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Synthesis of S-([18F]fluoromethyl)-(+)-McN5652 as a potential PET radioligand for the serotonin transporter.
- Source :
-
Nuclear medicine and biology [Nucl Med Biol] 2001 Oct; Vol. 28 (7), pp. 857-63. - Publication Year :
- 2001
-
Abstract
- 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).
- Subjects :
- Animals
Caudate Nucleus metabolism
Drug Stability
Fluorine Radioisotopes
In Vitro Techniques
Indicators and Reagents
Isotope Labeling
Magnetic Resonance Spectroscopy
Paroxetine metabolism
Radioligand Assay
Radiopharmaceuticals pharmacology
Serotonin Plasma Membrane Transport Proteins
Selective Serotonin Reuptake Inhibitors metabolism
Solvents
Swine
Tomography, Emission-Computed
Carrier Proteins metabolism
Isoquinolines chemical synthesis
Membrane Glycoproteins metabolism
Membrane Transport Proteins
Nerve Tissue Proteins
Radiopharmaceuticals chemical synthesis
Serotonin Antagonists chemical synthesis
Subjects
Details
- Language :
- English
- ISSN :
- 0969-8051
- Volume :
- 28
- Issue :
- 7
- Database :
- MEDLINE
- Journal :
- Nuclear medicine and biology
- Publication Type :
- Academic Journal
- Accession number :
- 11578908
- Full Text :
- https://doi.org/10.1016/s0969-8051(01)00248-7