These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


Pubmed for Handhelds

PUBMED FOR HANDHELDS

Search MEDLINE/PubMed

  • Title: Radiosynthesis of racemic and enantiomerically pure (-)-[18F]flubatine--a promising PET radiotracer for neuroimaging of α4β2 nicotinic acetylcholine receptors.
    Author: Fischer S, Hiller A, Smits R, Hoepping A, Funke U, Wenzel B, Cumming P, Sabri O, Steinbach J, Brust P.
    Journal: Appl Radiat Isot; 2013 Apr; 74():128-36. PubMed ID: 23416407.
    Abstract:
    (-)-[(18)F]flubatine is a promising agent for visualization by PET of cerebral α4β2 nicotinic acetylcholine receptors (nAChRs), which are implicated in psychiatric and neurodegenerative disorders. Here, we describe a substantially improved two-step radiosynthesis strategy for (-)-[(18)F]flubatine, based on the nucleophilic radiofluorination of an enantiomerically pure precursor followed by deprotection of the intermediate. An extensive leaving group/protecting group library of precursors was tested. Application of a trimethylammonium-iodide precursor with a Boc-protecting group provided the best results: labeling efficiencies of 80-95%, RCY of 60±5%, radiochemical purity of >98%, and a specific activity of >350GBq/μmol. The radiosynthesis is easily transferable to an automated synthesis module.
    [Abstract] [Full Text] [Related] [New Search]