Automated radiosynthesis of [18F]FBEM, a sulfhydryl site specific labeling agent for peptides and proteins

Appl Radiat Isot. 2018 Oct:140:294-299. doi: 10.1016/j.apradiso.2018.07.033. Epub 2018 Jul 29.

Abstract

In the process of developing [18F]FBEM coupled target peptide, we have instituted a robust automated synthesis of [18F]FBEM, a sulfhydryl (-SH) site specific agent for radiolabeling of peptides and proteins. The radiosynthesis generated 1.67-3.89 GBq (45.1-105.1 mCi, 7.5-18.8% non-decay corrected yield) of [18F]FBEM from 22.2 GBq (600 mCi) of starting [18F]fluoride with molar activity of 31.8 ± 5.3 GBq/µmol (0.86 ± 0.14 mCi/nmol) (n = 3) at the end of synthesis. Radiochemical purity was greater than 98%, and total synthesis time was ~90 min.

Keywords: Automation; PET; Radiotracer synthesis; Thiol(-SH)-specific; [(18)F]FBEM.

MeSH terms

  • Animals
  • Chromatography, High Pressure Liquid
  • Fluorine Radioisotopes / chemistry*
  • Glucagon-Like Peptide 1 / analogs & derivatives*
  • Glucagon-Like Peptide 1 / chemical synthesis
  • Glucagon-Like Peptide 1 / chemistry
  • Glucagon-Like Peptide 1 / standards
  • Maleimides / chemical synthesis*
  • Maleimides / chemistry*
  • Maleimides / standards
  • Peptides / chemistry
  • Proteins / chemistry
  • Quality Control
  • Radiochemistry / instrumentation
  • Radiochemistry / methods
  • Radiopharmaceuticals / chemical synthesis*
  • Radiopharmaceuticals / chemistry*
  • Radiopharmaceuticals / standards
  • Sulfhydryl Reagents / chemical synthesis
  • Sulfhydryl Reagents / chemistry

Substances

  • Fluorine Radioisotopes
  • Maleimides
  • N-2-(4-fluorobenzamido)ethylmaleimide-EM 3106B
  • Peptides
  • Proteins
  • Radiopharmaceuticals
  • Sulfhydryl Reagents
  • Glucagon-Like Peptide 1
  • Fluorine-18