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Items: 17


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.


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.


Direct one-step 18F-labeling of peptides via nucleophilic aromatic substitution.

Becaud J, Mu L, Karramkam M, Schubiger PA, Ametamey SM, Graham K, Stellfeld T, Lehmann L, Borkowski S, Berndorff D, Dinkelborg L, Srinivasan A, Smits R, Koksch B.

Bioconjug Chem. 2009 Dec;20(12):2254-61. doi: 10.1021/bc900240z.


Synthetic strategies to alpha-trifluoromethyl and alpha-difluoromethyl substituted alpha-amino acids.

Smits R, Cadicamo CD, Burger K, Koksch B.

Chem Soc Rev. 2008 Aug;37(8):1727-39. doi: 10.1039/b800310f. Epub 2008 Jun 26. Review.


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