Revisiting the Radiosynthesis of [ 18 F]FPEB and Preliminary PET Imaging in a Mouse Model of Alzheimer's Disease

[ F]FPEB is a positron emission tomography (PET) radiopharmaceutical used for imaging the abundance and distribution of mGluR5 in the central nervous system (CNS). Efficient radiolabeling of the aromatic ring of [ F]FPEB has been an ongoing challenge. Herein, five metal-free precursors for the radio...

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Veröffentlicht in:	Molecules (Basel, Switzerland) Switzerland), 2020-02, Vol.25 (4), p.982
Hauptverfasser:	Varlow, Cassis, Murrell, Emily, Holland, Jason P, Kassenbrock, Alina, Shannon, Whitney, Liang, Steven H, Vasdev, Neil, Stephenson, Nickeisha A
Format:	Artikel
Sprache:	eng
Schlagworte:	[18f]fpeb Alzheimer Disease - diagnostic imaging Alzheimer Disease - genetics Alzheimer Disease - pathology Alzheimer's disease alzheimer’s disease (ad) Amyloid beta-Protein Precursor - genetics Amyloid precursor protein Animals Aromatic compounds Automation Brain research Central nervous system Central Nervous System - diagnostic imaging Central Nervous System - metabolism Communication Computed tomography Disease Disease Models, Animal Fluorides Fluorine isotopes Fluorodeoxyglucose F18 - chemistry Fluorodeoxyglucose F18 - pharmacology Glutamic acid receptors (metabotropic) Humans iodonium-ylide Medical imaging mglur5 Mice Mice, Transgenic Neuroimaging Oligopeptides - genetics Pharmaceuticals Positron emission Positron emission tomography positron emission tomography (pet) Positron-Emission Tomography - methods Post traumatic stress disorder Precursors Presenilin 1 Radiochemistry Radioisotopes Radiopharmaceuticals - pharmacology Receptor, Metabotropic Glutamate 5 - chemistry Receptor, Metabotropic Glutamate 5 - genetics Receptor, Metabotropic Glutamate 5 - isolation & purification Sport utility vehicles Sulfonium salts Tomography
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Beschreibung
Zusammenfassung:	[ F]FPEB is a positron emission tomography (PET) radiopharmaceutical used for imaging the abundance and distribution of mGluR5 in the central nervous system (CNS). Efficient radiolabeling of the aromatic ring of [ F]FPEB has been an ongoing challenge. Herein, five metal-free precursors for the radiofluorination of [ F]FPEB were compared, namely, a chloro-, nitro-, sulfonium salt, and two spirocyclic iodonium ylide (SCIDY) precursors bearing a cyclopentyl (SPI5) and a new adamantyl (SPIAd) auxiliary. The chloro- and nitro-precursors resulted in a low radiochemical yield (
ISSN:	1420-3049 1420-3049
DOI:	10.3390/molecules25040982