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[18F]FE@SNAP—A new PET tracer for the melanin concentrating hormone receptor 1 (MCHR1): Microfluidic and vessel-based approaches
- Source :
- Bioorganic & Medicinal Chemistry. 20(19):5936-5940
- Publication Year :
- 2012
- Publisher :
- Elsevier BV, 2012.
-
Abstract
- Changes in the expression of the melanin concentrating hormone receptor 1 (MCHR1) are involved in a variety of pathologies, especially obesity and anxiety disorders. To monitor these pathologies in-vivo positron emission tomography (PET) is a suitable method. After the successful radiosynthesis of [11C]SNAP-7941—the first PET-Tracer for the MCHR1, we aimed to synthesize its [18F]fluoroethylated analogue: [18F]FE@SNAP. Therefore, microfluidic and vessel-based approaches were tested. [18F]fluoroethylation was conducted via various [18F]fluoroalkylated synthons and direct [18F]fluorination. Only the direct [18F]fluorination of a tosylated precursor using a flow-through microreactor was successful, affording [18F]FE@SNAP in 44.3±2.6%.
- Subjects :
- Clinical Biochemistry
Microfluidics
Radioligand
Pharmaceutical Science
Biochemistry
03 medical and health sciences
0302 clinical medicine
SNAP-7941
Drug Discovery
Receptor
Molecular Biology
030304 developmental biology
Medicine(all)
0303 health sciences
MCHR1
Chemistry
Organic Chemistry
Radiosynthesis
Snap
Combinatorial chemistry
Fluorine-18
3. Good health
Melanin-concentrating hormone receptor
PET
Microfluidic
Molecular Medicine
Microreactor
030217 neurology & neurosurgery
Subjects
Details
- ISSN :
- 09680896
- Volume :
- 20
- Issue :
- 19
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry
- Accession number :
- edsair.doi.dedup.....1ff71e80424d809fb1d18210c442769e
- Full Text :
- https://doi.org/10.1016/j.bmc.2012.07.051