Rapid and reproducible radiosynthesis of [18F] FHBG

Nucl Med Biol. 2004 Jan;31(1):133-8. doi: 10.1016/s0969-8051(03)00096-9.

Abstract

9-(4-[18F] Fluoro-3-hydroxymethylbutyl) guanine ([18F] FHBG), an imaging agent for gene therapy using PET, was prepared in a one-pot, two-step synthesis. Microwave (MW) mediated nucleophilic fluorination of N2, monomethoxytrityl-9-[4-(tosyl)-3-monomethoxytrityl-methylbutyl] guanine using no-carrier-added [18F] fluoride, followed by deprotection with hydrochloric acid and HPLC purification, gave [18F] FHBG. The radiochemical yield (decay corrected) was 12+/-5% (n = 35), the synthesis time was 55-60 min, and the radiochemical purity was >99%. The compound was used for lung imaging and was injected into Sprague-Dawley rats previously infected with the herpes simplex virus type 1 thymidine kinase (HSV1-tk) reporter gene. MicroPET imaging showed accumulation confined to the lungs.

Publication types

  • Comparative Study
  • Evaluation Study
  • Research Support, U.S. Gov't, P.H.S.
  • Validation Study

MeSH terms

  • Animals
  • Guanine / analogs & derivatives*
  • Guanine / chemistry*
  • Guanine / pharmacokinetics*
  • Lung / diagnostic imaging*
  • Lung / metabolism*
  • Radiopharmaceuticals / chemical synthesis
  • Radiopharmaceuticals / pharmacokinetics
  • Rats
  • Rats, Sprague-Dawley
  • Reproducibility of Results
  • Sensitivity and Specificity
  • Thymidine Kinase / genetics
  • Thymidine Kinase / metabolism*
  • Tissue Distribution
  • Tomography, Emission-Computed / methods
  • Viral Proteins / genetics
  • Viral Proteins / metabolism*

Substances

  • 9-(4-fluoro-3-hydroxymethylbutyl)guanine
  • Radiopharmaceuticals
  • Viral Proteins
  • Guanine
  • thymidine kinase, Canid herpesvirus 1
  • Thymidine Kinase