86656-36-2Relevant articles and documents
Exploration of alcohol-enhanced Cu-mediated radiofluorination toward practical labeling
Zhou, Dong,Chu, Wenhua,Katzenellenbogen, John A.
, p. 13 - 20 (2021/10/23)
Copper-mediated nucleophilic radiofluorination using boronic precursors is a promising, general method to label aromatic compounds with [18F]fluoride. However, in various reports, large amounts of precursor (60 μmol) were needed to achieve high
Synthesis, radiofluorination, and preliminary evaluation of the potential 5-HT2A receptor agonists [18F]Cimbi-92 and [18F]Cimbi-150
Edgar, Fraser Graeme,Hansen, Hanne D.,Leth-Petersen, Sebastian,Ettrup, Anders,Kristensen, Jesper L.,Knudsen, Gitte M.,Herth, Matthias M.
, p. 586 - 591 (2017/10/07)
An agonist PET tracer is of key interest for the imaging of the 5-HT2A receptor, as exemplified by the previously reported success of [11C]Cimbi-36. Fluorine-18 holds several advantages over carbon-11, making it the radionuclide of choice for clinical purposes. In this respect, an 18F-labelled agonist 5-HT2A receptor (5-HT2AR) tracer is highly sought after. Herein, we report a 2-step, 1-pot labelling methodology of 2 tracer candidates. Both ligands display high in vitro affinities for the 5-HT2AR. The compounds were synthesised from easily accessible labelling precursors, and radiolabelled in acceptable radiochemical yields, sufficient for in vivo studies in domestic pigs. PET images partially conformed to the expected brain distribution of the 5-HT2AR; a notable exception however being significant uptake in the striatum and thalamus. Additionally, a within-scan displacement challenge with a 5-HT2AR antagonist was unsuccessful, indicating that the tracers cannot be considered optimal for neuroimaging of the 5-HT2AR.
Neither azeotropic drying, nor base nor other additives: A minimalist approach to 18F-labeling
Richarz,Krapf,Zarrad,Urusova,Neumaier,Zlatopolskiy
supporting information, p. 8094 - 8099 (2015/01/08)
A novel, efficient, time-saving and reliable radiolabeling procedure via nucleophilic substitution with [18F]fluoride is described. Different radiolabeled aliphatic and aromatic compounds were prepared in high radiochemical yields simply by hea
