- Synthesis of [¹¹C]PBR170, a novel imidazopyridine, for imaging the translocator protein with PET.
Synthesis of [¹¹C]PBR170, a novel imidazopyridine, for imaging the translocator protein with PET.
Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine (2014-04-02)
Thomas Bourdier, David Henderson, Christopher J R Fookes, Peter Lam, Filomena Mattner, Michael Fulham, Andrew Katsifis
PMID24685494
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.
MATERIALS
Product Number
Brand
Product Description
Sigma-Aldrich
Acetonitrile solution, contains 0.1 % (v/v) trifluoroacetic acid, suitable for HPLC
Supelco
Residual Solvent - Acetonitrile(solution in DMSO), Pharmaceutical Secondary Standard; Certified Reference Material
Sigma-Aldrich
Acetonitrile solution, contains 10.0% acetone, 0.05% formic acid, 40.0% 2-propanol
Sigma-Aldrich
Acetonitrile solution, contains 0.05 % (w/v) ammonium formate, 5 % (v/v) water, 0.1 % (v/v) formic acid, suitable for HPLC