Literature DB >> 17448665

Synthesis procedure for routine production of 2-[18F]fluoro-3-(2(S)-azetidinylmethoxy)pyridine (2-[18F]F-A-85380).

Andreas Schildan1, Marianne Patt, Osama Sabri.   

Abstract

2-[18F]Fluoro-3-(2(S)-azetidinylmethoxy)pyridine (2-[18F]F-A-85380) was among the first subtype selective radioligands to visualise the in vivo distribution of alpha4beta2-containing neuronal nicotinic acetylcholine receptors (nAChRs) in human brain. We developed a one-pot synthesis for the preparation of 2-[18F]F-A-85380 in a commercially available TRACERlab FXF-N synthesis module. The synthesis comprises a nucleophilic substitution followed by hydrolysis of a t-butyloxycarbonyl (BOC)-protected intermediate. After formulation for intravenous application up to 20 G Bq 2-[18F]F-A-85380 were produced from a starting activity of 100 G Bq [18F]fluoride in 60 min with a specific activity of about 4.10(5)GBq/mmol and a mean radiochemical purity of more than 99%.

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Year:  2007        PMID: 17448665     DOI: 10.1016/j.apradiso.2007.02.009

Source DB:  PubMed          Journal:  Appl Radiat Isot        ISSN: 0969-8043            Impact factor:   1.513


  4 in total

1.  Positron emission tomography experience with 2-[¹⁸F]fluoro-3-(2(S)-azetidinylmethoxy)pyridine (2-[¹⁸F]FA) in the living human brain of smokers with paranoid schizophrenia.

Authors:  James Robert Brašić; Nicola Cascella; Anil Kumar; Yun Zhou; John Hilton; Vanessa Raymont; Andrew Crabb; Maria Rita Guevara; Andrew G Horti; Dean Foster Wong
Journal:  Synapse       Date:  2011-12-29       Impact factor: 2.562

2.  Decreased cerebral α4β2* nicotinic acetylcholine receptor availability in patients with mild cognitive impairment and Alzheimer's disease assessed with positron emission tomography.

Authors:  Kai Kendziorra; Henrike Wolf; Philipp Mael Meyer; Henryk Barthel; Swen Hesse; Georg Alexander Becker; Julia Luthardt; Andreas Schildan; Marianne Patt; Dietlind Sorger; Anita Seese; Herman-Josef Gertz; Osama Sabri
Journal:  Eur J Nucl Med Mol Imaging       Date:  2010-11-11       Impact factor: 9.236

3.  Single photon emission computed tomography experience with (S)-5-[(123)I]iodo-3-(2-azetidinylmethoxy)pyridine in the living human brain of smokers and nonsmokers.

Authors:  James Robert Brasić; Yun Zhou; John L Musachio; John Hilton; Hong Fan; Andrew Crabb; Christopher J Endres; Melvin J Reinhardt; Ahmet S Dogan; Mohab Alexander; Olivier Rousset; Marika A Maris; Jeffrey Galecki; Ayon Nandi; Dean F Wong
Journal:  Synapse       Date:  2009-04       Impact factor: 2.562

4.  Automated synthesis of an 18F-labelled pyridine-based alkylating agent for high yield oligonucleotide conjugation.

Authors:  Elisabeth von Guggenberg; Jayden A Sader; John S Wilson; Soraya Shahhosseini; Ingrid Koslowsky; Frank Wuest; John R Mercer
Journal:  Appl Radiat Isot       Date:  2009-04-19       Impact factor: 1.513

  4 in total

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