[18F]DPA-714, [18F]PBR111 and [18F]FEDAA1106-selective radioligands for imaging TSPO 18 kDa with PET: automated radiosynthesis on a TRACERLAb FX-FN synthesizer and quality controls

Appl Radiat Isot. 2012 Mar;70(3):489-97. doi: 10.1016/j.apradiso.2011.10.015. Epub 2011 Nov 11.

Abstract

Imaging of TSPO 18 kDa with PET is more and more considered as a relevant biomarker of inflammation in numerous diseases. Development of new radiotracers for TSPO 18 kDa has seen acceleration in the last years and the challenge today is to make available large amounts of such a radiotracer in compliance with GMP standards for application in humans. We present in this technical note automated productions of [(18)F]DPA-714, [(18)F]PBR111 and [(18)F]FEDAA1106, three promising radiotracers for TSPO 18 kDa imaging, using a TRACERlab FX-FN synthesizer. This note also includes the quality control data of the validation batches for the manufacturing qualification of clinical production of [(18)F]DPA-714.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetamides / chemistry*
  • Fluorine Radioisotopes / chemistry*
  • Magnetic Resonance Spectroscopy
  • Positron-Emission Tomography*
  • Pyrazoles / chemistry*
  • Pyridines / chemistry*
  • Pyrimidines / chemistry*
  • Quality Control
  • Radioligand Assay
  • Receptors, GABA / chemistry*

Substances

  • 2-(6-chloro-2-(4-(3-fluoropropoxy)phenyl)imidazo(1,2-a)pyridin-3-yl)-N,N-diethylacetamide
  • Acetamides
  • Bzrp protein, mouse
  • Fluorine Radioisotopes
  • N,N-diethyl-2-(2-(4-(2-fluoroethoxy)phenyl)-5,7-dimethylpyrazolo(1,5-a)pyrimidin-3-yl)acetamide
  • N-(5-fluoro-2-phenoxyphenyl)-N-(2-fluoroethyl-5-methoxybenzyl)acetamide
  • Pyrazoles
  • Pyridines
  • Pyrimidines
  • Receptors, GABA