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In vitro and in vivo Human Metabolism of (S)-[18F]Fluspidine - A Radioligand for Imaging σ1 Receptors With Positron Emission Tomography (PET).

Ludwig FA, Fischer S, Houska R, Hoepping A, Deuther-Conrad W, Schepmann D, Patt M, Meyer PM, Hesse S, Becker GA, Zientek FR, Steinbach J, Wünsch B, Sabri O, Brust P.

Front Pharmacol. 2019 Jun 13;10:534. doi: 10.3389/fphar.2019.00534. eCollection 2019.


Image-Guided Development of Heterocyclic Sulfoxides as Ligands for Tau Neurofibrillary Tangles: From First-in-Man to Second-Generation Ligands.

Rafique W, Kramer V, Pardo T, Smits R, Spilhaug MM, Hoepping A, Savio E, Engler H, Kuljs R, Amaral H, Riss PJ.

ACS Omega. 2018 Jul 31;3(7):7567-7579. doi: 10.1021/acsomega.8b00975. Epub 2018 Jul 9.


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

Sabri O, Meyer PM, Gräf S, Hesse S, Wilke S, Becker GA, Rullmann M, Patt M, Luthardt J, Wagenknecht G, Hoepping A, Smits R, Franke A, Sattler B, Tiepolt S, Fischer S, Deuther-Conrad W, Hegerl U, Barthel H, Schönknecht P, Brust P.

Brain. 2018 Jun 1;141(6):1840-1854. doi: 10.1093/brain/awy099.


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

Ludwig FA, Fischer S, Smits R, Deuther-Conrad W, Hoepping A, Tiepolt S, Patt M, Sabri O, Brust P.

Molecules. 2018 Feb 20;23(2). pii: E464. doi: 10.3390/molecules23020464.


Procedures for the GMP-Compliant Production and Quality Control of [18F]PSMA-1007: A Next Generation Radiofluorinated Tracer for the Detection of Prostate Cancer.

Cardinale J, Martin R, Remde Y, Schäfer M, Hienzsch A, Hübner S, Zerges AM, Marx H, Hesse R, Weber K, Smits R, Hoepping A, Müller M, Neels OC, Kopka K.

Pharmaceuticals (Basel). 2017 Sep 27;10(4). pii: E77. doi: 10.3390/ph10040077.


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

Kranz M, Sattler B, Tiepolt S, Wilke S, Deuther-Conrad W, Donat CK, Fischer S, Patt M, Schildan A, Patt J, Smits R, Hoepping A, Steinbach J, Sabri O, Brust P.

EJNMMI Phys. 2016 Dec;3(1):25. Epub 2016 Oct 21.


Enhanced copper-mediated (18)F-fluorination of aryl boronic esters provides eight radiotracers for PET applications.

Preshlock S, Calderwood S, Verhoog S, Tredwell M, Huiban M, Hienzsch A, Gruber S, Wilson TC, Taylor NJ, Cailly T, Schedler M, Collier TL, Passchier J, Smits R, Mollitor J, Hoepping A, Mueller M, Genicot C, Mercier J, Gouverneur V.

Chem Commun (Camb). 2016 Jun 28;52(54):8361-4. doi: 10.1039/c6cc03295h.


Development of a Novel Nonpeptidic (18)F-Labeled Radiotracer for in Vivo Imaging of Oxytocin Receptors with Positron Emission Tomography.

Wenzel B, Mollitor J, Deuther-Conrad W, Dukic-Stefanovic S, Kranz M, Vraka C, Teodoro R, Günther R, Donat CK, Ludwig FA, Fischer S, Smits R, Wadsak W, Mitterhauser M, Steinbach J, Hoepping A, Brust P.

J Med Chem. 2016 Mar 10;59(5):1800-17. doi: 10.1021/acs.jmedchem.5b01080. Epub 2016 Feb 3.


Radiosynthesis and first preclinical evaluation of the novel norepinephrine transporter pet-ligand [(11)C]ME@HAPTHI.

Rami-Mark C, Berroterán-Infante N, Philippe C, Foltin S, Vraka C, Hoepping A, Lanzenberger R, Hacker M, Mitterhauser M, Wadsak W.

EJNMMI Res. 2015 Dec;5(1):113. doi: 10.1186/s13550-015-0113-3. Epub 2015 Jun 10.


First-in-human PET quantification study of cerebral α4β2* nicotinic acetylcholine receptors using the novel specific radioligand (-)-[(18)F]Flubatine.

Sabri O, Becker GA, Meyer PM, Hesse S, Wilke S, Graef S, Patt M, Luthardt J, Wagenknecht G, Hoepping A, Smits R, Franke A, Sattler B, Habermann B, Neuhaus P, Fischer S, Tiepolt S, Deuther-Conrad W, Barthel H, Schönknecht P, Brust P.

Neuroimage. 2015 Sep;118:199-208. doi: 10.1016/j.neuroimage.2015.05.065. Epub 2015 May 30.


Internal dose assessment of (-)-18F-flubatine, comparing animal model datasets of mice and piglets with first-in-human results.

Sattler B, Kranz M, Starke A, Wilke S, Donat CK, Deuther-Conrad W, Patt M, Schildan A, Patt J, Smits R, Hoepping A, Schoenknecht P, Steinbach J, Brust P, Sabri O.

J Nucl Med. 2014 Nov;55(11):1885-92. doi: 10.2967/jnumed.114.137059. Epub 2014 Oct 6.


Evaluation of metabolism, plasma protein binding and other biological parameters after administration of (-)-[(18)F]Flubatine in humans.

Patt M, Becker GA, Grossmann U, Habermann B, Schildan A, Wilke S, Deuther-Conrad W, Graef S, Fischer S, Smits R, Hoepping A, Wagenknecht G, Steinbach J, Gertz HJ, Hesse S, Schönknecht P, Brust P, Sabri O.

Nucl Med Biol. 2014 Jul;41(6):489-94. doi: 10.1016/j.nucmedbio.2014.03.018. Epub 2014 Mar 29.


Synthesis and biological evaluation of both enantiomers of [(18)F]flubatine, promising radiotracers with fast kinetics for the imaging of α4β2-nicotinic acetylcholine receptors.

Smits R, Fischer S, Hiller A, Deuther-Conrad W, Wenzel B, Patt M, Cumming P, Steinbach J, Sabri O, Brust P, Hoepping A.

Bioorg Med Chem. 2014 Jan 15;22(2):804-12. doi: 10.1016/j.bmc.2013.12.011. Epub 2013 Dec 12.


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

Patt M, Schildan A, Habermann B, Fischer S, Hiller A, Deuther-Conrad W, Wilke S, Smits R, Hoepping A, Wagenknecht G, Steinbach J, Brust P, Sabri O.

Appl Radiat Isot. 2013 Oct;80:7-11. doi: 10.1016/j.apradiso.2013.05.009. Epub 2013 Jun 7.


Radiosynthesis of racemic and enantiomerically pure (-)-[18F]flubatine--a promising PET radiotracer for neuroimaging of α4β2 nicotinic acetylcholine receptors.

Fischer S, Hiller A, Smits R, Hoepping A, Funke U, Wenzel B, Cumming P, Sabri O, Steinbach J, Brust P.

Appl Radiat Isot. 2013 Apr;74:128-36. doi: 10.1016/j.apradiso.2013.01.002. Epub 2013 Jan 11.


GABAA receptor pharmacology of fluorinated derivatives of the novel sedative-hypnotic pyrazolopyrimidine indiplon.

Wegner F, Deuther-Conrad W, Scheunemann M, Brust P, Fischer S, Hiller A, Diekers M, Strecker K, Wohlfarth K, Allgaier C, Steinbach J, Hoepping A.

Eur J Pharmacol. 2008 Feb 2;580(1-2):1-11. Epub 2007 Oct 22.


Synthesis of fluorine substituted pyrazolopyrimidines as potential leads for the development of PET-imaging agents for the GABAA receptors.

Hoepping A, Diekers M, Deuther-Conrad W, Scheunemann M, Fischer S, Hiller A, Wegner F, Steinbach J, Brust P.

Bioorg Med Chem. 2008 Feb 1;16(3):1184-94. Epub 2007 Nov 26.


Radiosynthesis and biological evaluation of an 18F-labeled derivative of the novel pyrazolopyrimidine sedative-hypnotic agent indiplon.

Hoepping A, Scheunemann M, Fischer S, Deuther-Conrad W, Hiller A, Wegner F, Diekers M, Steinbach J, Brust P.

Nucl Med Biol. 2007 Jul;34(5):559-70. Epub 2007 Jun 8.


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