A high yield robotic synthesis of 9-(4-[18F]-fluoro-3-hydroxymethylbutyl)guanine ([18F]FHBG) and 9-[3-[18F]fluoro-1-hydroxy-2-propoxy)methyl]guanine([18F] FHPG) for gene expression imaging

Appl Radiat Isot. 2007 Jan;65(1):57-63. doi: 10.1016/j.apradiso.2006.06.005. Epub 2006 Aug 17.

Abstract

The aim of this study was to develop an automated synthesis of 9-(4-[(18)F]-fluoro-3-hydroxymethylbutyl)guanine ([(18)F]FHBG) and 9-[(3-[(18)F]fluoro-1-hydroxy-2-propoxy)methyl]guanine ([(18)F]FHPG) using a Scanditronix Anatech RB III robotic system. [(18)F]HF was produced via (18)O(p, n)(18)F using a Scanditronix MC17F cyclotron. On average, a typical run produced [(18)F]FHBG and [(18)F]FHPG with an uncorrected radiochemical yield of 19% and 16%, respectively, at end of synthesis (EOS) from irradiation of 95% enriched [(18)O]water. The total synthesis time was 80 min. The retention time of [(18)F]FHBG and [(18)F]FHPG (the radio-peak) was 3.9 and 4.0 min, respectively, which was consistent with the [(19)F]FHBG and [(19)F]FHPG ultraviolet peak. The radiochemical purity was greater than 97%. A robotic, automated method for [(18)F]FHBG and [(18)F]FHPG radiosynthesis is therefore feasible. The radiation burden for the operator can be reduced as much as possible. Sufficient radioactivities of [(18)F]FHBG and [(18)F]FHPG could be obtained for non-invasive monitoring the expression of transfected gene in vivo with positron emission tomography (PET).

Publication types

  • Evaluation Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Equipment Design
  • Equipment Failure Analysis
  • Ganciclovir / analogs & derivatives*
  • Ganciclovir / chemical synthesis
  • Ganciclovir / isolation & purification
  • Gene Expression Profiling / instrumentation
  • Gene Expression Profiling / methods*
  • Guanine / analogs & derivatives*
  • Guanine / chemical synthesis
  • Guanine / isolation & purification
  • Isotope Labeling / instrumentation*
  • Isotope Labeling / methods
  • Molecular Probe Techniques
  • Positron-Emission Tomography / instrumentation
  • Positron-Emission Tomography / methods*
  • Radiopharmaceuticals / chemical synthesis
  • Robotics / instrumentation*
  • Robotics / methods
  • Specimen Handling / instrumentation*
  • Specimen Handling / methods

Substances

  • 9-((3-fluoro-1-hydroxy-2-propoxy)methyl)guanine
  • 9-(4-fluoro-3-hydroxymethylbutyl)guanine
  • Radiopharmaceuticals
  • Guanine
  • Ganciclovir