Radiosynthesis of [18F]AV1451 in pharmaceutical conditions and its biological characteristics

Appl Radiat Isot. 2017 Oct:128:101-107. doi: 10.1016/j.apradiso.2017.06.032. Epub 2017 Jun 30.

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.

MeSH terms

  • Blood Proteins / metabolism
  • Carbolines / blood
  • Carbolines / chemical synthesis*
  • Carbolines / chemistry
  • Chromatography, High Pressure Liquid
  • Fluorine Radioisotopes / chemistry*
  • Humans
  • Lipoproteins / metabolism
  • Neurodegenerative Diseases / blood
  • Neurodegenerative Diseases / diagnostic imaging
  • Protein Binding
  • Radioligand Assay
  • Radiopharmaceuticals / blood
  • Radiopharmaceuticals / chemical synthesis*
  • Radiopharmaceuticals / chemistry
  • Reproducibility of Results
  • Spectrophotometry, Ultraviolet

Substances

  • Blood Proteins
  • Carbolines
  • Fluorine Radioisotopes
  • Lipoproteins
  • Radiopharmaceuticals
  • 7-(6-fluoropyridin-3-yl)-5H-pyrido(4,3-b)indole