Literature DB >> 23792828

Fully automated radiosynthesis of both enantiomers of [18F]Flubatine under GMP conditions for human application.

Marianne Patt1, Andreas Schildan, Bernd Habermann, Steffen Fischer, Achim Hiller, Winnie Deuther-Conrad, Stephan Wilke, René Smits, Alexander Hoepping, Gudrun Wagenknecht, Jörg Steinbach, Peter Brust, Osama Sabri.   

Abstract

A fully automatized radiosynthesis of (+)- and (-)-[(18)F]Flubatine ((+)- and (-)NCFHEB) by means of a commercially available synthesis module (TRACERlab FX FN) under GMP conditions is reported. Radiochemical yields of 30% within an overall synthesis time of 40 min were achieved in more than 70 individual syntheses. Specific activities were approximately 3000 GBq/μmol and radiochemical purity was determined to be at least 97%.
Copyright © 2013 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Automation; Flubatine; Fluorine-18; GMP; NCFHEB; α(4)β(2) Nicotinic acetylcholine receptors

Mesh：

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Year:  2013        PMID： 23792828     DOI： 10.1016/j.apradiso.2013.05.009

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


  7 in total

Review 1.  Development of (18)F-labeled radiotracers for neuroreceptor imaging with positron emission tomography.

Authors:  Peter Brust; Jörg van den Hoff; Jörg Steinbach
Journal:  Neurosci Bull       Date:  2014-08-29       Impact factor: 5.203

2.  Evaluation of [(18)F]-(-)-norchlorofluorohomoepibatidine ([(18)F]-(-)-NCFHEB) as a PET radioligand to image the nicotinic acetylcholine receptors in non-human primates.

Authors:  Frederic Bois; Jean-Dominique Gallezot; Ming-Qiang Zheng; Shu-Fei Lin; Irina Esterlis; Kelly P Cosgrove; Richard E Carson; Yiyun Huang
Journal:  Nucl Med Biol       Date:  2014-08-08       Impact factor: 2.408

3.  Quinuclidine and DABCO Enhance the Radiofluorinations of 5-Substituted 2-Halopyridines.

Authors:  Gregory R Naumiec; Lisheng Cai; Shuiyu Lu; Victor W Pike
Journal:  European J Org Chem       Date:  2017-09-04

4.  Evaluation of the sensitivity of the novel α4β2* nicotinic acetylcholine receptor PET radioligand 18F-(-)-NCFHEB to increases in synaptic acetylcholine levels in rhesus monkeys.

Authors:  Jean-Dominique Gallezot; Irina Esterlis; Frederic Bois; Ming-Qiang Zheng; Shu-Fei Lin; Tracy Kloczynski; John H Krystal; Yiyun Huang; Osama Sabri; Richard E Carson; Kelly P Cosgrove
Journal:  Synapse       Date:  2014-07-28       Impact factor: 2.562

5.  Radiation dosimetry of the α4β2 nicotinic receptor ligand (+)-[18F]flubatine, comparing preclinical PET/MRI and PET/CT to first-in-human PET/CT results.

Authors:  Mathias Kranz; Bernhard Sattler; Solveig Tiepolt; Stephan Wilke; Winnie Deuther-Conrad; Cornelius K Donat; Steffen Fischer; Marianne Patt; Andreas Schildan; Jörg Patt; René Smits; Alexander Hoepping; Jörg Steinbach; Osama Sabri; Peter Brust
Journal:  EJNMMI Phys       Date:  2016-10-21

6.  Cognitive correlates of α4β2 nicotinic acetylcholine receptors in mild Alzheimer's dementia.

Authors:  Osama Sabri; Philipp M Meyer; Susanne Gräf; Swen Hesse; Stephan Wilke; Georg-Alexander Becker; Michael Rullmann; Marianne Patt; Julia Luthardt; Gudrun Wagenknecht; Alexander Hoepping; Rene Smits; Annegret Franke; Bernhard Sattler; Solveig Tiepolt; Steffen Fischer; Winnie Deuther-Conrad; Ulrich Hegerl; Henryk Barthel; Peter Schönknecht; Peter Brust
Journal:  Brain       Date:  2018-06-01       Impact factor: 13.501

7.  Exploring the Metabolism of (+)-[18F]Flubatine in Vitro and in Vivo: LC-MS/MS Aided Identification of Radiometabolites in a Clinical PET Study.

Authors:  Friedrich-Alexander Ludwig; Steffen Fischer; René Smits; Winnie Deuther-Conrad; Alexander Hoepping; Solveig Tiepolt; Marianne Patt; Osama Sabri; Peter Brust
Journal:  Molecules       Date:  2018-02-20       Impact factor: 4.411
  7 in total

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