Abstract
In this study, we describe the radiosynthesis of [18F]AV1451 in terms of its pharmaceutical quality and characterise its physical and biological properties. We performed an in vitro serum stability study in fresh human plasma and a plasma protein binding study. The radiochemical yield was 24% (decay corrected), and the product met all regulatory quality requirements. We found that this compound is stable in fresh human plasma and binds tightly to plasma proteins, especially lipoproteins.
Keywords:
Neurodegeneration; Plasma protein binding; Radiopharmaceutical drug; TAU protein.
Copyright © 2017 Elsevier Ltd. All rights reserved.
MeSH terms
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Blood Proteins / metabolism
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Carbolines / blood
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Carbolines / chemical synthesis*
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Carbolines / chemistry
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Chromatography, High Pressure Liquid
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Fluorine Radioisotopes / chemistry*
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Humans
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Lipoproteins / metabolism
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Neurodegenerative Diseases / blood
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Neurodegenerative Diseases / diagnostic imaging
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Protein Binding
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Radioligand Assay
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Radiopharmaceuticals / blood
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Radiopharmaceuticals / chemical synthesis*
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Radiopharmaceuticals / chemistry
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Reproducibility of Results
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Spectrophotometry, Ultraviolet
Substances
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Blood Proteins
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Carbolines
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Fluorine Radioisotopes
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Lipoproteins
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Radiopharmaceuticals
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7-(6-fluoropyridin-3-yl)-5H-pyrido(4,3-b)indole