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Appl Radiat Isot. 2016 Aug;114:57-62. doi: 10.1016/j.apradiso.2016.04.028. Epub 2016 Apr 28.

Tos-Nos-Mos: Synthesis of different aryl sulfonate precursors for the radiosynthesis of the alpha7 nicotinic acetylcholine receptor radioligand [(18)F]NS14490.

Author information

1
Helmholtz-Zentrum Dresden - Rossendorf, Institute of Radiopharmaceutical Cancer Research, Departments of Neuroradiopharmaceuticals and Radiopharmaceutical and Chemical Biology, POB 51 01 19, D-01314 Dresden, Germany.
2
DanPET AB, Rosenstigen 7, SE-216 19 Malmö, Sweden.
3
Helmholtz-Zentrum Dresden - Rossendorf, Institute of Radiopharmaceutical Cancer Research, Departments of Neuroradiopharmaceuticals and Radiopharmaceutical and Chemical Biology, POB 51 01 19, D-01314 Dresden, Germany. Electronic address: s.fischer@hzdr.de.

Abstract

Radiopharmacological investigations of [(18)F]NS14490 have proven that this radiotracer could be a potential PET radiotracer for imaging of alpha7 nicotinic acetylcholine receptor particularly with regard to vulnerable plaques of diseased vessels. For further optimisation of the previously automated one-pot radiosynthesis of [(18)F]NS14490 using a tosylate precursor, precursors with other leaving groups (nosylate and mosylate) were synthesized and compared with the tosylate with respect to their reactivities towards [(18)F]fluoride. The use of these different precursors resulted in comparable labelling yields of [(18)F]NS14490. A novel mosylate precursor was synthesized and evaluated, which has revealed a higher stability during a storage period of five months compared to the corresponding tosylate and nosylate.

KEYWORDS:

Alpha7 nAChR ligand; Mosylate; Nosylate; PET; Reactivity of precursor; Synthesis of precursor; Tosylate

PMID:
27183376
DOI:
10.1016/j.apradiso.2016.04.028
[Indexed for MEDLINE]

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