Radiosynthesis and validation of [5-cyano-N-(4-(4-[11 C]methylpiperazin-1-yl)-2-(piperidin-1-yl)phenyl) furan-2-carboxamide] ([11 C]CPPC), a PET radiotracer for imaging CSF1R, a microglia-specific marker

J Labelled Comp Radiopharm. 2019 Nov;62(13):903-908. doi: 10.1002/jlcr.3806. Epub 2019 Nov 6.

Abstract

In this practitioner protocol, the radiochemical synthesis of [11 C]CPPC is described in detail, and a quality control summary of three validation productions is presented. The results indicate that the radiotracer product can be produced in good radiochemical yield (> 60 mCi (2.22 GBq) at end-of-synthesis (EOS)), at high specific activity (molar activity > 11,435 mCi/μmole (423 GBq/μmole) at EOS) and high chemical and radiochemical purity. The entire production conforms to current Good Manufacturing Practice (cGMP) requirements. The final product is formulated as a sterile, pyrogen-free solution suitable for human injection.

Keywords: CPPC; CSF1R; PET; QC; synthesis.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Biomarkers / metabolism
  • Chemistry Techniques, Synthetic
  • Furans / chemical synthesis*
  • Furans / chemistry*
  • Microglia / metabolism*
  • Positron-Emission Tomography / methods*
  • Quality Control
  • Radiochemistry
  • Receptors, Granulocyte-Macrophage Colony-Stimulating Factor / metabolism*

Substances

  • Biomarkers
  • Furans
  • Receptors, Granulocyte-Macrophage Colony-Stimulating Factor