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Appl Radiat Isot. 2014 Aug;90:46-52. doi: 10.1016/j.apradiso.2014.03.009. Epub 2014 Mar 18.

Synthesis of [¹¹C]PBR170, a novel imidazopyridine, for imaging the translocator protein with PET.

Author information

  • 1Department of PET and Nuclear Medicine, Royal Prince Alfred Hospital, Missenden Road, Camperdown NSW 2050, Australia. Electronic address: thomas@nucmed.rpa.cs.nsw.gov.au.
  • 2Department of PET and Nuclear Medicine, Royal Prince Alfred Hospital, Missenden Road, Camperdown NSW 2050, Australia.
  • 3LifeSciences, Australian Nuclear Science and Technology Organisation, Locked Bag 2001, Kirrawee DC NSW 2232, Australia.
  • 4Department of PET and Nuclear Medicine, Royal Prince Alfred Hospital, Missenden Road, Camperdown NSW 2050, Australia; Sydney Medical School, University of Sydney, Camperdown NSW 2050, Australia.

Abstract

The translocator protein (TSPO) ligand 2-(6,8-dichloro-2-(4-ethoxyphenyl)imidazo[1,2-a]pyridin-3-yl)-N-(2-fluoropyridin-3-yl)-N-methylacetamide (PBR170), is a novel imidazopyridineacetamide with high affinity (2.6 nm) and selectivity for the TSPO. The synthesis of [(11)C]PBR170 was accomplished by N-methylation of the corresponding desmethyl precursor with [(11)C]methyl iodide in the presence of sodium hydroxide in dimethylformamide. [(11)C]PBR170 was produced in 30-45% radiochemical yield (decay-corrected, based on [(11)C]methyl iodide) with a radiochemical purity >98% and a specific activity of 90-190 GBq/μmol after 35 min of synthesis time.

KEYWORDS:

Carbon-11; PET; TSPO; [(11)C]PBR170; [(11)C]methyl iodide

PMID:
24685494
DOI:
10.1016/j.apradiso.2014.03.009
[PubMed - indexed for MEDLINE]
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