Fully automated radiosynthesis of [ 11C]PBR28, a radiopharmaceutical for the translocator protein (TSPO) 18kDa, using a GE TRACERlab FX C-Pro

Applied Radiation and Isotopes

Volumn 70, Issue 8, 2012, Pages 1779-1783

  Hoareau, Raphaël ^a   Shao, Xia ^a   Henderson, Bradford D ^a   Scott, Peter J H ^a  

^a UNIVERSITY OF MICHIGAN MEDICAL SCHOOL   (United States)

Author keywords

11C PBR28; Microglial activation; Peripheral benzodiazepine receptor (PBR); Positron emission tomography; Radiopharmaceutical synthesis

Indexed keywords

[ 11C]PBR28; CHEMICAL PURITY; HIGH QUALITY; ONE-POT SYNTHESIS; PERIPHERAL BENZODIAZEPINE RECEPTOR (PBR); PET IMAGING; RADIOCHEMICAL YIELD; RADIOLABELLING; RADIOSYNTHESIS; SOLID-PHASE EXTRACTION; SPECIFIC ACTIVITY; TRANSLOCATORS;

OPTIMIZATION;

POSITRON EMISSION TOMOGRAPHY;

ALCOHOL; CARRIER PROTEIN; N (2 METHOXYBENZYL) N (4 PHENOXY 3 PYRIDINYL)ACETAMIDE C 11; PBR 28; RADIOPHARMACEUTICAL AGENT; SODIUM CHLORIDE; UNCLASSIFIED DRUG;

ARTICLE; AUTOMATION; DRUG STRUCTURE; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; ISOTOPE LABELING; ONE POT SYNTHESIS; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; PROCESS OPTIMIZATION; PROTEIN ANALYSIS; PURIFICATION; QUALITY CONTROL; RADIATION DOSE; RADIOCHEMISTRY; SOLID PHASE EXTRACTION;

ACETAMIDES; AUTOMATION; CARBON RADIOISOTOPES; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; PYRIDINES; QUALITY CONTROL; RADIOPHARMACEUTICALS; RECEPTORS, GABA;

EID: 84863775118     PISSN: 09698043     EISSN: 18729800     Source Type: Journal    
DOI: 10.1016/j.apradiso.2012.03.006     Document Type: Article

References (9)

1. Bae J.W., Cho Y.J., Lee S.H., Yoon C.-O.M., Yoon C.M. Chem. Commun. 2000, 1857-1858.
2. Briard E., Zoghbi S.S., Imaizumi M., Gourley J.P., Shetty H.U., Hong J., Cropley V., Fujita M., Innis R.B., Pike V.W. Synthesis and evaluation in monkey of two sensitive 11C-labeled aryloxyanilide ligands for imaging brain peripheral benzodiazepine receptors in vivo. J. Med. Chem. 2008, 51:17-30.
3. Brown A.K., Fujita M., Fujimura Y., Liow J.-S., Stabin M., Ryu Y.H., Imaizumi M., Hong J., Pike V.W., Innis R.B. J. Nucl. Med. 2007, 2072-2079.
4. 11C]PBR28, a PET biomarker for the peripheral benzodiazepine receptor. Tetrahedron Lett. 2010, 51:3353-3355.
5. Imaizumi M., Kim H.-J., Zoghbi S.S., Briard E., Hong J., Musachio J.L., Ruetzler C., Chuang D.-M., Pike V.W., Innis R.B., Fujita M. PET imaging with [11C]PBR28 can localize and quantify upregulated peripheral benzodiazepine receptors associated with cerebral ischemia in rat. Neurosci. Lett. 2007, 411:200-205.
6. Papadopoulos V., Baraldi M., Guilarte T.R., Knudsen T.B., Lacapere J.-J., Lindemann P., Norenberg M.D., Nutt D., Weizman A., Zhang M.-R., Gavish M. Translocator protein (18kDa): new nomenclature for the peripheral-type benzodiazepine receptor based on its structure and molecular function. Trends Pharmacol. Sci. 2006, 27:402-409.
7. Shao, X., Hoareau, R., Runkle, A.C., Tluczek, L.J.M., Hockley, B.G., Henderson, B.D., Scott, P.J.H., 2011. Highlighting the versatility of the TRACERlab synthesis modules. Part 2: fully automated production of [11C] labeled radiopharmaceuticals using a TRACERlab FXC-Pro. J. Labelled Compd. Radiopharm. 54, 819-838.
8. Venneti S., Lopresti B.J., Wiley C.A. The peripheral benzodiazepine receptor (translocator protein 18kDa) in microglia: from pathology to imaging. Prog. Neurobiol. 2006, 80:308-322.
9. 11C]PBR28. Bioorg. Med. Chem. Lett. 2009, 19:5636-5639.