Publications of Institute of Radiopharmaceutical Cancer Research

189 Publications

2021

Pathophysiological Changes in the Enteric Nervous System of Rotenone-Exposed Mice as Early Radiological Markers for Parkinson's Disease

Schaffernicht, G.; Shang, Q.; Stievenard, A.; Bötzel, K.; Dening, Y.; Kempe, R.; Toussaint, M.; Gündel, D.; Kranz, M.; Reichmann, H.; Vanbesien-Mailliot, C.; Brust, P.; Dieterich, M.; Funk, R. H. W.; Ravens, U.; Pan-Montojo, F.


Synthesis of novel fluorinated xanthine derivatives with high adenosine A2B receptor binding affinity

Lindemann, M.; Dukic-Stefanovic, S.; Hinz, S.; Deuther-Conrad, W.; Teodoro, R.; Juhl, C.; Steinbach, J.; Brust, P.; Müller, C. E.; Wenzel, B.


Design, radiosynthesis and preliminary biological evaluation in mice of a brain-penetrant 18F-labelled σ2 receptor ligand

Moldovan, R.-P.; Gündel, D.; Teodoro, R.; Ludwig, F.-A.; Fischer, S.; Toussaint, M.; Schepmann, D.; Wünsch, B.; Brust, P.; Deuther-Conrad, W.


Challenges on cyclic nucleotide phosphodiesterases imaging with positron emission tomography: Novel radioligands and (pre-)clinical insights since 2016

Schröder, S.; Scheunemann, M.; Wenzel, B.; Brust, P.


Validation of an LC-MS/MS method to quantify the new TRPC6 inhibitor SH045 (larixyl N-methylcarbamate) and its application in an exploratory pharmacokinetic study in mice

Chai, X.-N.; Ludwig, F.-A.; Müglitz, A.; Schaefer, M.; Yin, H.-Y.; Brust, P.; Regenthal, R.; Krügel, U.


Preclinical evaluation of [18F]FACH in healthy mice and piglets: An 18F-labeled ligand for imaging of monocarboxylate transporters with PET

Gündel, D.; Sadeghzadeh, M.; Deuther-Conrad, W.; Wenzel, B.; Cumming, P.; Toussaint, M.; Ludwig, F.-A.; Moldovan, R.-P.; Kranz, M.; Teodoro, R.; Sattler, B.; Sabri, O.; Brust, P.


Synthesis and biological evaluation of a novel 18F-labeled radiotracer for PET imaging of the adenosine A2A receptor

Lai, T. H.; Toussaint, M.; Teodoro, R.; Dukic-Stefanovic, S.; Kranz, M.; Deuther-Conrad, W.; Moldovan, R.-P.; Brust, P.


Development of 18F-labeled radiotracers for PET imaging of the adenosine A2A receptor: Synthesis, radiolabeling and preliminary biological evaluation

Lai, T. H.; Schröder, S.; Toussaint, M.; Dukic-Stefanovic, S.; Kranz, M.; Ludwig, F.-A.; Fischer, S.; Steinbach, J.; Deuther-Conrad, W.; Brust, P.; Moldovan, R.-P.


Improved in vivo PET imaging of the adenosine A2A receptor in the brain using [18F]FLUDA, a deuterated radiotracer with high metabolic stability

Lai, T. H.; Toussaint, M.; Teodoro, R.; Dukic-Stefanovic, S.; Gündel, D.; Ludwig, F.-A.; Wenzel, B.; Schröder, S.; Sattler, B.; Moldovan, R.-P.; Falkenburger, B. H.; Sabri, O.; Deuther-Conrad, W.; Brust, P.


Studies on the affinity of 6-[(: N -(cyclo)aminoalkyl)oxy]-4 H -chromen-4-ones for sigma 1/2 receptors

Deuther-Conrad, W.; Diez-Iriepa, D.; Iriepa, I.; López-Muñoz, F.; Martínez-Grau, A. M.; Gütschow, M.; Marco-Contelles, J.


Sigma-1 and dopamine D2/D3 receptor occupancy of pridopidine in healthy volunteers and patients with Huntington disease: a [18F] fluspidine and [18F] fallypride PET study

Grachev, I.; Meyer, P.; Becker, G.; Bronzel, M.; Marsteller, D.; Pastino, G.; Voges, O.; Rabinovich, L.; Knebel, H.; Zientek, F.; Rullmann, M.; Sattler, B.; Patt, M.; Gerhards, T.; Strauss, M.; Kluge, A.; Brust, P.; Savola, J.; Gordon, M.; Geva, M.; Hesse, S.; Barthel, H.; Hayden, M.; Sabri, O.


(+)-[18F]Flubatine as a novel α4β2 nicotinic acetylcholine receptor PET ligand – Results of the first-in-human brain imaging application in patients with β-amyloid PET-confirmed Alzheimer’s disease and healthy controls

Tiepolt, S.; Becker, G.-A.; Wilke, S.; Cecchin, D.; Rullmann, M.; Meyer, P. M.; Barthel, H.; Hesse, S.; Patt, M.; Luthardt, J.; Wagenknecht, G.; Sattler, B.; Deuther-Conrad, W.; Ludwig, F.-A.; Fischer, S.; Gertz, H.-J.; Smits, R.; Hoepping, A.; Steinbach, J.; Brust, P.; Sabri, O.


2020

In silico finding of key interaction mediated α3β4 and α7 nicotinic acetylcholine receptor ligand selectivity of quinuclidine-triazole chemotype

Arunrungvichian, K.; Chongruchiroj, S.; Sarasamkan, J.; Schüürmann, G.; Brust, P.; Vajragupta, O.


Adenosine/A2B Receptor Signaling Ameliorates the Effects of Aging and Counteracts Obesity

Gnad, T.; Navarro, G.; Lahesmaa, M.; Reverte-Salisa, L.; Copperi, F.; Cordomi, A.; Naumann, J.; Hochh€Auser, A.; Haufs-Brusberg, S.; Wenzel, D.; Suhr, F.; Zenius Jespersen, N.; Scheele, C.; Tsvilovskyy, V.; Brinkmann, C.; Rittweger, J.; Dani, C.; Kranz, M.; Deuther-Conrad, W.; Eltzschig, H. K.; Niemi, T.; Taittonen, M.; Brust, P.; Nuutila, P.; Pardo, L.; Fleischmann, B. K.; Bleuher, M.; Franco, R.; Bloch, W.; Virtanen, K. A.; Pfeifer, A.


Sigma-1 Receptor Positron Emission Tomography: A New Molecular Imaging Approach Using ( S)-(-)-[ 18 F]Fluspidine in Glioblastoma

Toussaint, M.; Deuther-Conrad, W.; Kranz, M.; Fischer, S.; Ludwig, F.-A.; Juratli, T.; Patt, M.; Wünsch, B.; Schackert, G.; Sabri, O.; Brust, P.


Synthesis and evaluation of new 1-oxa-8-azaspiro[4.5]decane derivatives as candidate radioligands for sigma-1 receptors

Tian, J.; He, Y.; Deuther-Conrad, W.; Fu, H.; Xie, F.; Zhang, Y.; Wang, T.; Zhang, X.; Zhang, J.; Brust, P.; Huang, Y.; Jia, H.


Development of a radiofluorinated adenosine A2B receptor antagonist as potential ligand for PET imaging

Lindemann, M.; Moldovan, R.-P.; Hinz, S.; Deuther-Conrad, W.; Gündel, D.; Dukic-Stefanovic, S.; Toussaint, M.; Teodoro, R.; Juhl, C.; Steinbach, J.; Brust, P.; Müller, C. E.; Wenzel, B.


Development of novel analogs of the monocarboxylate transporter ligand FACH and biological validation of one potential radiotracer for PET imaging

Sadeghzadeh, M.; Wenzel, B.; Gündel, D.; Deuther-Conrad, W.; Toussaint, M.; Moldovan, R.-P.; Fischer, S.; Teodoro, R.; Jonnalagadda, S.; Jonnalagadda, S. K.; Mereddy, V. R.; Drewes, L. R.; Brust, P.


Preclinical incorporation dosimetry of [18F]FACH - a novel 18F-labeled MCT1/MCT4 lactate transporter inhibitor for imaging cancer metabolism with PET

Sattler, B.; Kranz, M.; Wenzel, B.; Thachaantara Jain, N.; Moldovan, R.-P.; Toussaint, M.; Deuther-Conrad, W.; Ludwig, F.-A.; Teodoro, R.; Sattler, T.; Sadeghzadeh, M.; Sabri, O.; Brust, P.


The sigma-1 receptor: potential role in the modulation of cellular radiation sensitivity

Belter, B.; Deuther-Conrad, W.; Hofheinz, F.; Bachmann, M.; Brust, P.; Pietzsch, J.


Newly synthesized fluorinated cinnamylpiperazines possessing low in vitro MAO-B binding

Jevtić, I. I.; Lai, T. H.; Penjišević, J. Z.; Dukic-Stefanovic, S.; Andrić, D. B.; Brust, P.; Kostić-Rajačić, S. V.; Teodoro, R.


PET Imaging of the Adenosine A2A Receptor in the Rotenone-Based Mouse Model of Parkinson’s Disease with [18F]FESCH Synthesized by a Simplified Two-Step One-Pot Radiolabeling Strategy

Schröder, S.; Lai, T. H.; Toussaint, M.; Kranz, M.; Chovsepian, A.; Shang, Q.; Dukic-Stefanovic, S.; Deuther-Conrad, W.; Teodoro, R.; Wenzel, B.; Moldovan, R.-P.; Pan-Montojo, F.; Brust, P.


2019

Radiosynthesis and Biological Investigation of a Novel Fluorine-18 Labeled Benzoimidazotriazine- based Radioligand for Imaging of Phosphodiesterase 2A with Positron Emission Tomography

Ritawidya, R.; Wenzel, B.; Teodoro, R.; Toussaint, M.; Kranz, M.; Deuther-Conrad, W.; Dukic-Stefanovic, S.; Ludwig, F.-A.; Scheunemann, M.; Brust, P.


One-step radiosynthesis of the MCTs imaging agent [18F]FACH by aliphatic 18F-labelling of a methylsulfonate precursor containing an unprotected carboxylic acid group

Sadeghzadeh, M.; Moldovan, R.-P.; Teodoro, R.; Brust, P.; Wenzel, B.


Structure–Affinity Relationships of Fluorinated Spirocyclic Sigma2 Receptor Ligands with an Exocyclic Benzylamino Moiety

Bergkemper, M.; Kronenberg, E.; Schepmann, D.; Ludwig, F.-A.; Brust, P.; Wünsch, B.


¹⁸F-Labeled benzylpiperazine derivatives as highly selective ligands for imaging σ1 receptor with positron emission tomography

Ye, J.; Wang, L.; Deuther-Conrad, W.; Chen, Y.; Zhang, X.; Zhang, J.; Huang, Y.; Brust, P.; Jia, H.

  • Journal of Labelled Compounds and Radiopharmaceuticals 62(2019)8, 425-437
    DOI: 10.1002/jlcr.3738

Synthesis and in vitro evaluation of 8-pyridinyl substituted benzo[e]imidazo[2,1-c][1,2,4]triazines as phosphodiesterase 2A (PDE2A) inhibitors

Ritawidya, R.; Ludwig, F.-A.; Briel, D.; Brust, P.; Scheunemann, M.


SPECT-Untersuchungen mit dem 123 I-markierten Dopamintransporter-Liganden FP-CIT (DaTSCAN):DGN-Handlungsempfehlung (S1-Leitlinie)

Tatsch, K.; Buchert, R.; Bartenstein, P.; Barthel, H.; Boecker, H.; Brust, P.; Drzezga, A.; La Fougère, C.; Gründer, G.; Grünwald, F.; Krause, B.-J.; Kuwert, T.; Langen, K.-J.; Rominger, A.; Sabri, O.; Schreckenberger, M.; Meyer, P. T.

  • Nuklearmedizin 58(2019)1, 5-16

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

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


Development and radiosynthesis of the first 18F-labeled inhibitor of monocarboxylate transporters (MCTs)

Sadeghzadeh, M.; Moldovan, R.-P.; Fischer, S.; Wenzel, B.; Ludwig, F.-A.; Teodoro, R.; Deuther-Conrad, W.; Jonnalagadda, S.; K. Jonnalagadda, S.; Gudelis, E.; Šačkus, A.; R. Mereddy, V.; R. Drewes, L.; Brust, P.

  • Open Access Logo Journal of Labelled Compounds and Radiopharmaceuticals 62(2019)8, 411-424
    DOI: 10.1002/jlcr.3739

Targeting cyclic nucleotide phosphodiesterase 5 (PDE5) in brain: Toward the development of a PET radioligand labeled with fluorine-18

Wenzel, B.; Liu, J.; Dukic-Stefanovic, S.; Deuther-Conrad, W.; Teodoro, R.; Ludwig, F.-A.; Chezal, J.-M.; Moreau, E.; Brust, P.; Maisonial-Besset, A.


Studies towards the development of a PET radiotracer for imaging of the P2Y1 receptors in the brain: synthesis, 18F-labeling and preliminary biological evaluation

Moldovan, R.-P.; Wenzel, B.; Teodoro, R.; Neumann, W.; Dukic-Stefanovic, S.; Deuther-Conrad, W.; Hey-Hawkins, E.; Krügel, U.; Brust, P.


2018

Synthesis, Receptor Affinity, and Antiallodynic Activity of Spirocyclic σ Receptor Ligands with Exocyclic Amino Moiety

Bergkemper, M.; Kronenberg, E.; Thum, S.; Börgel, F.; Daniliuc, C.; Schepmann, D.; Nieto, F. R.; Brust, P.; Reinoso, R. F.; Alvarez, I.; Wünsch, B.


Fourier Analysis of Cerebral Metabolism of Glucose: Gender Differences in Mechanisms of Color Processing in the Ventral and Dorsal Streams in Mice

Njemanze, P. C.; Kranz, M.; Brust, P.


Contilisant, a Tetratarget Small Molecule for Alzheimer’s Disease Therapy Combining Cholinesterase, Monoamine Oxidase Inhibition and H3R Antagonism with Sigma 1R Agonism Profile

Bautista-Aguilera, O. M.; Budni, J.; Mina, F.; Medeiros, E. B.; Deuther-Conrad, W.; Entrena, J. M.; Moraleda, I.; Iriepa, I.; López-Muñoz, F.; Marco-Contelles, J.


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

Sabri, O.; Meyer, P. M.; Gräf, S.; Hesse, S.; Wilke, S.; Becker, G.-A.; 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.


Radiosynthesis and in vivo evaluation of a fluorine-18 labeled pyrazine based radioligand for PET imaging of the adenosine A2B receptor

Lindemann, M.; Hinz, S.; Deuther-Conrad, W.; Namasivayam, V.; Dukic-Stefanovic, S.; Teodoro, R.; Toussaint, M.; Kranz, M.; Juhl, C.; Steinbach, J.; Brust, P.; Müller, C. E.; Wenzel, B.


Synthesis and radiofluorination of novel fluoren-9-one based derivatives for the imaging of α7 nicotinic acetylcholine receptor with PET

Teodoro, R.; Scheunemann, M.; Wenzel, B.; Peters, D.; Deuther-Conrad, W.; Brust, P.


Exploring the Metabolism of (+)-[18F]Flubatine in vitro and in vivo: LC-MS/MS aided Identification of Radiometabolites in a Clinical PET Study

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


Investigation of an 18F-labelled Imidazopyridotriazine for Molecular Imaging of Cyclic Nucleotide Phosphodiesterase 2A

Schröder, S.; Wenzel, B.; Deuther-Conrad, W.; Teodoro, R.; Kranz, M.; Scheunemann, M.; Egerland, U.; Höfgen, N.; Briel, D.; Steinbach, J.; Brust, P.


Bridging from Brain to Tumor imaging: (S)- and (R)-[18F]Fluspidine for investigation of Sigma-1 Receptors in Tumor-bearing Mice

Kranz, M.; Bergmann, R.; Kniess, T.; Belter, B.; Neuber, C.; Cai, Z.; Deng, G.; Fischer, S.; Steinbach, J.; Zhou, J.; Huang, H.; Brust, P.; Deuther-Conrad, W.; Pietzsch, J.


2017

Maternal immune activation results in complex microglial transcriptome signature in the adult offspring that is reversed by minocycline treatment

Mattei, D.; Ivanov, A.; Ferrai, C.; Jordan, P.; Guneykaya, D.; Buonfiglioli, A.; Schaafsma, W.; Przanowski, P.; Deuther-Conrad, W.; Brust, P.; Hesse, S.; Patt, M.; Sabri, O.; Ross, T. L.; Eggen, B. J. L.; Bodecke, E. W. G. M.; Kaminska, B.; Beule, D.; Pombo, A.; Kettenmann, H.; Wolf, S. A.


PET Imaging Evaluation of Four sigma1 Radiotracers in Nonhuman Primates

Baum, E.; Cai, Z.; Bois, F.; Holden, D.; Lin, S.-F.; Lara-Jaime, T.; Kapinos, M.; Chen, Y.; Deuther-Conrad, W.; Fischer, S.; Dukic-Stefanovic, S.; Bunse, P.; Wünsch, B.; Brust, P.; Jia, H.; Huang, Y.


1‑(4‑[18F]Fluorobenzyl)-4-[(tetrahydrofuran-2-yl)methyl]piperazine: A Novel Suitable Radioligand with Low Lipophilicity for Imaging σ1 Receptors in the Brain

He, Y.; Xie, F.; Ye, J.; Deuther-Conrad, W.; Cui, B.; Wang, L.; Lu, J.; Steinbach, J.; Brust, P.; Huang, Y.; Lu, J.; Jia, H.


18F-Labeled indole-based analogs as highly selective radioligands for imaging sigma-2 receptors in the brain

Wang, L.; Ye, J.; He, Y.; Deuther-Conrad, W.; Zhang, J.; Zhang, X.; Cui, M.; Steinbach, J.; Huang, Y.; Brust, P.; Jia, H.


Synthesis and in vitro evaluation of 5-substituted benzovesamicol analogs containing N-substituted amides as potential positron emission tomography tracers for the vesicular acetylcholine transporter

Roslin, S.; de Rosa, M.; Deuther-Conrad, W.; Eriksson, J.; Odell, L. R.; Antoni, G.; Brust, P.; Larhed, M.


Radiosynthesis of (S)-[18F]T1: The first PET radioligand for molecular imaging of α3β4 nicotinic acetylcholine receptors

Sarasamkan, J.; Fischer, S.; Deuther-Conrad, W.; Ludwig, F.-A.; Scheunemann, M.; Arunrungvichian, K.; Vajragupta, O.; Brust, P.


Do spiroindolines have the potential to replace vesamicol as lead compound for the development of radioligands targeting the vesicular acetylcholine transporter?

Lindemann, M.; Deuther-Conrad, W.; Moldovan, R.; Sekhar, K. V. G. C.; Brust, P.; Wenzel, B.


Development of highly affine and selective fluorinated cannabinoid receptor type 2 ligands

Moldovan, R.-P.; Hausmann, K.; Deuther-Conrad, W.; Brust, P.


Development of Fluorinated Non-Peptidic Ghrelin Receptor Ligands for Potential Use in Molecular Imaging

Moldovan, R.-P.; Els-Heindl, S.; Worm, D. J.; Kniess, T.; Kluge, M.; Beck-Sickinger, A. G.; Deuther-Conrad, W.; Krügel, U.; Brust, P.


PET Imaging of α7 Nicotinic Acetylcholine Receptors: A comparative study of [18F]ASEM and [18F]DBT-10 in non-human primates, and further evaluation of [18F]ASEM in humans

Hillmer, A. T.; Li, S.; Zheng, M.-Q.; Scheunemann, M.; Lin, S.-F.; Nabulsi, N.; Holden, D.; Pracitto, R.; Labaree, D.; Ropchan, J.; Teodoro, R.; Deuther-Conrad, W.; Esterlis, I.; Cosgrove, K. P.; Carson, R. E.; Brust, P.; Huang, Y.


Suppressed Fat Appetite after Roux-en-Y Gastric Bypass Surgery Associates with Reduced Brain µ-opioid Receptor Availability in Diet-Induced Obese Male Rats

Hankir, M.; Patt, M.; Patt, J.; Becker, G.; Rullmann, M.; Kranz, M.; Deuther-Conrad, W.; Schichke, K.; Seyfried, F.; Brust, P.; Hesse, S.; Sabri, O.; Krügel, U.; Fenske, W.


Synthesis and in vitro evaluation of new fluorinated quinoline derivatives with high affinity for PDE5: Towards the development of new PET neuroimaging probes

Liu, J.; Maisonial-Besset, A.; Wenzel, B.; Canitrot, D.; Baufond, A.; Chezal, J. M.; Brust, P.; Moreau, E.


Gender Differences in Neural Networks for Color Processing in Mice: A PET/MR Study

Njemanze, P. C.; Kranz, M.; Amend, M.; Wehrl, H.; Brust, P.


Dissociation between brown adipose tissue 18F-FDG uptake and thermogenesis in uncoupling protein deficient mice

Hankir, M. K.; Kranz, M.; Keipert, S.; Andreasen, S.; Kern, M.; Patt, M.; Klöting, N.; Hesse, S.; Brust, P.; Jastroch, M.; Fenske, W. K.


Synthesis and Preliminary Biological Evaluation of Indol-3-yl-oxoacetamides as Potent Cannabinoid Receptor Type 2 Ligands

Moldovan, R.-P.; Deuther-Conrad, W.; Horti, A. G.; Brust, P.


Gastric Bypass Surgery Recruits a Gut – Striatal Dopamine Pathway to Reduce Fat Appetite in Obese Rats

Hankir, M. K.; Seyfried, F.; Hintschich, C. A.; Diep, T. A.; Kleberg, K.; Kranz, M.; Deuther-Conrad, W.; Tellez, L. A.; Rullmann, M.; Patt, M.; Teichert, S.; Sabri, O.; Brust, P.; Hansen, H. S.; de Araujo, I. E.; Krügel, U.; Fenske, W. K.


Radiosynthesis and biological evaluation of the new PDE10A radioligand [18F]AQ28A

Wagner, S.; Teodoro, R.; Deuther-Conrad, W.; Kranz, M.; Scheunemann, M.; Fischer, S.; Wenzel, B.; Egerland, U.; Hoefgen, N.; Steinbach, J.; Brust, P.

  • Open Access Logo Journal of Labelled Compounds and Radiopharmaceuticals 60(2017)1, 36-48
    DOI: 10.1002/jlcr.3471

2016

Targetting microglia activation in schizophrenia by minocycline treatment

Mattei, D.; Ivanov, A.; Ferrai, G.; Jordan, P.; Guneykaya, D.; Schaafsma, W.; Przanowski, P.; Deuther-Conrad, W.; Brust, P.; Hesse, S.; Eggen, B.; Bodekke, E.; Kaminska, B.; Pombo, A.; Kettenmann, H.; Wolf, S. A.

  • Lecture (Conference)
    29th ECNP Congress, 17.-20.09.2016, Vienna, Österreich
  • European Neuropsychopharmacology 26(2016), 134

Evaluation of the enantiomer specific biokinetics and radiation doses of [18-F]-fluspidine – a new tracer in clinical translation for imaging of σ1 receptors

Kranz, M.; Sattler, B.; Wüst, N.; Deuther-Conrad, W.; Patt, M.; Meyer, P. M.; Fischer, S.; Donat, C. K.; Wünsch, B.; Hesse, S.; Steinbach, J.; Brust, P.; Sabri, O.


Synthesis and evaluation of a 18F-labeled 4-phenylpiperidine-4-carbonitrile radioligand for σ1 receptor imaging

Ye, J.; Wang, X.; Deuther-Conrad, W.; Zhang, J.; Li, J.; Zhang, X.; Wang, L.; Steinbach, J.; Brust, P.; Jia, H.

  • Open Access Logo Journal of Labelled Compounds and Radiopharmaceuticals (2016), 332-339
    DOI: 10.1002/jlcr.3408

Tos-Nos-Mos: Synthesis of different aryl sulfonate precursors for the radiosynthesis of the alpha7 nicotinic acetylcholine receptor radioligand [18F]NS14490

Rötering, S.; Scheunemann, M.; Günther, R.; Löser, R.; Hiller, A.; Peters, D.; Brust, P.; Fischer, S.; Steinbach, J.


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, C.; Fischer, S.; Patt, M.; Schildan, A.; Patt, J.; Smits, R.; Hoepping, A.; Steinbach, J.; Sabri, O.; Brust, P.


Novel radioligands for cyclic nucleotide phosphodiesterase imaging with positron emission tomography: An update on developments since 2012

Schröder, S.; Wenzel, B.; Deuther-Conrad, W.; Scheunemann, M.; Brust, P.


Varying Chirality Across Nicotinic Acetylcholine Receptor Subtypes: Selective Binding of Quinuclidine Triazole Compounds

Sarasamkan, J.; Scheunemann, M.; Apaijai, N.; Palee, S.; Parichatikanond, W.; Arunrungvichian, K.; Fischer, S.; Chattipakorn, S.; Deuther-Conrad, W.; Schüürmann, G.; Brust, P.; Vajragupta, O.


Comparison of in silico, electrochemical, in vitro and in vivo metabolism of a homologous series of (radio)fluorinated sigma1 receptor ligands designed for positron emission tomography

Wiese, C.; Große Maestrup, E.; Galla, F.; Schepmann, D.; Hiller, A.; Fischer, S.; Ludwig, F. A.; Deuther-Conrad, W.; Donat, C. K.; Brust, P.; Büter, L.; Karst, U.; Wünsch, B.


Beta-Amyloid-PET-Bildgebung des Gehirns - DGN-Handlungsempfehlung

Barthel, H.; Meyer, P. T.; Drzezga, A.; Bartenstein, P.; Boecker, H.; Brust, P.; Buchert, R.; Coenen, H. H.; Fougère, C. L.; Gründer, G.; Grünwald, F.; Krause, B. J.; Kuwert, T.; Schreckenberger, M.; Tatsch, K.; Langen, K. J.; Sabri, O.


99mTc-Cyclopentadienyl Tricarbonyl Chelate-Labeled Compounds as Selective Sigma‑2 Receptor Ligands for Tumor Imaging

Li, D.; Chen, Y.; Wang, X.; Deuther-Conrad, W.; Chen, X.; Jia, B.; Dong, C.; Steinbach, J.; Brust, P.; Liu, B.; Jia, H.


LC-MS supported Studies on the in vitro Metabolism of both Enantiomers of Flubatine and the in vivo Metabolism of (+)-[18F]Flubatine – a Positron Emission Tomography Radioligand for Imaging α4β2-Nicotinic Acetylcholine Receptors

Ludwig, F.-A.; Smits, R.; Fischer, S.; Donat, C. K.; Hoepping, A.; Brust, P.; Steinbach, J.


Thyroid hormone status defines brown adipose tissue activity and browning of white adipose tissues in mice

Weiner, J.; Kranz, M.; Klöting, N.; Kunath, A.; Steinhoff, K.; Rijntjes, E.; Köhrle, J.; Zeisig, V.; Hankir, M.; Gebhardt, C.; Deuther-Conrad, W.; Heiker, J.; Kralisch, S.; Stumvoll, M.; Bluher, M.; Sabri, O.; Hesse, S.; Brust, P.; Tönjes, A.; Krause, K.


Changes in Binding of [123I]CLINDE, a High-Affinity Translocator Protein 18 kDa (TSPO) Selective Radioligand in a Rat Model of Traumatic Brain Injury

Donat, C. K.; Gaber, K.; Meixensberger, J.; Brust, P.; Pinborg, L. H.; Hansen, H. H.; Mikkelsen, J. D.


Development of a High-Affinity PET Radioligand for Imaging Cannabinoid Subtype 2 Receptor

Moldovan, R.-P.; Teodoro, R.; Deuther-Conrad, W.; Kranz, M.; Wang, Y.; Nakano, M.; Valentine, H.; Fischer, S.; Pomper, M.; Wong, D. F.; Dannals, R. F.; Brust, P.; Horti, A. G.


Development of a new radiofluorinated quinoline analog for PET imaging of phosphodiesterase 5 (PDE5) in brain.

Liu, J.; Wenzel, B.; Dukic-Stefanovic, S.; Teodoro, R.; Ludwig, F.-A.; Deuther-Conrad, W.; Schröder, S.; Chezal, J.-M.; Moreau, E.; Brust, P.; Maisonial-Besset, A.


PET imaging evaluation of [18F]DBT-10, a novel radioligand specific to α7 nicotinic acetylcholine receptors, in nonhuman primates

Hillmer, A. T.; Zheng, M.-Q.; Li, S.; Scheunemann, M.; Lin, S.-F.; Holden, D.; Labaree, D.; Ropchan, J.; Teodoro, R.; Deuther-Conrad, W.; Carson, R. E.; Brust, P.; Huang, Y.


A novel thermoregulatory role for PDE10A in mouse and human adipocytes

Hankir, M.; Kranz, M.; Gnad, T.; Wagner, S.; Deuther-Conrad, W.; Bronisch, F.; Steinhoff, K.; Luthardt, J.; Klöting, N.; Hesse, S.; Seibyl, J.; Blüher, M.; Sabri, O.; Pfeifer, A.; Brust, P.; Fenske, W.


Development of highly potent phosphodiesterase 10A (PDE10A) inhibitors: Synthesis and in vitro evaluation of 1,8-dipyridyl- and 1-pyridinol-substituted imidazo[1,5-a]quinoxalines

Wagner, S.; Scheunemann, M.; Dipper, K.; Egerland, U.; Hoefgen, N.; Steinbach, J.; Brust, P.


On the development of a novel non-peptidic 18F-labeled radiotracer for in vivo imaging of oxytocin receptors with positron emission tomography

Wenzel, B.; Mollitor, J.; Deuther-Conrad, W.; Kranz, M.; Dukic-Stefanovic, S.; Günther, R.; Teodoro, R.; Ludwig, F.-A.; Fischer, S.; Smits, R.; Steinbach, J.; Hoepping, A.; Brust, P.

  • Poster
    ISRS2015 - 21st International Symposium on Radiopharmaceutical Sciences, 26.-31.05.2015, Columbia, Missouri, USA
  • Open Access Logo Abstract in refereed journal
    Journal of Labelled Compounds and Radiopharmaceuticals 58(2015)1, 173
    DOI: 10.1002/jlcr.3302_2
  • Journal of Medicinal Chemistry 59(2016)5, 1800-1817
    DOI: 10.1021/acs.jmedchem.5b01080

2015

18F-Labeled 1,4-Dioxa-8-azaspiro[4.5]decane Derivative: Synthesis and Biological Evaluation of a σ1 Receptor Radioligand with Low Lipophilicity as Potent Tumor Imaging Agent

Xie, F.; Bergmann, R.; Kniess, T.; Deuther-Conrad, W.; Mamat, C.; Neuber, C.; Liu, B.; Steinbach, J.; Brust, P.; Pietzsch, J.; Jia, H.


2-[18F]Fluoroethyl tosylate - a versatile tool for building 18F-based radiotracers for positron emission tomography

Knieß, T.; Laube, M.; Brust, P.; Steinbach, J.


Novel indole-based sigma-2 receptor ligands: synthesis, structure–affinity relationship and antiproliferative activity

Xie, F.; Kniess, T.; Neuber, C.; Deuther-Conrad, W.; Mamat, C.; Liebermann, B. P.; Liu, B.; Mach, R. H.; Brust, P.; Steinbach, J.; Pietzsch, J.; Jia, H.


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

Sabri, O.; Becker, G.-A.; Meyer, P. M.; 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.


A promising PET tracer for imaging of α7 nicotinic acetylcholine receptors in the brain: Design, synthesis, and in vivo evaluation of a dibenzothiophene-based radioligand

Teodoro, R.; Scheunemann, M.; Deuther-Conrad, W.; Wenzel, B.; Colombo, S.; Gotti, C.; Kranz, M.; Donat, C.; Patt, M.; Hillmer, A.; Zheng, M.; Peters, D.; Steinbach, J.; Sabri, O.; Huang, Y.; Brust, P.


Synthesis, 18F-radiolabelling and biological characterization of novel fluoroalkylated triazine derivatives for in vivo imaging of phosphodiesterase 2A in brain via positron emission tomography

Schröder, S.; Wenzel, B.; Deuther-Conrad, W.; Teodoro, R.; Egerland, U.; Kranz, M.; Scheunemann, M.; Höfgen, N.; Steinbach, J.; Brust, P.


New systematically modified vesamicol analogs and their affinity and selectivity for the vesicular acetylcholine transporter – A critical examination of the lead structure.

Barthel, C.; Sorger, D.; Deuther-Conrad, W.; Scheunemann, M.; Schweiger, S.; Jäckel, P.; Roghani, A.; Steinbach, J.; Schüürmann, G.; Sabri, O.; Brust, P.; Wenzel, B.


A high-yield automated radiosynthesis of the alpha-7 nicotinic receptor radioligand [18F]NS10743

Teodoro, R.; Wenzel, B.; Oh-Nishi, A.; Fischer, S.; Peters, D.; Suhara, T.; Deuther-Conrad, W.; Brust, P.


Convenient recycling and reuse of bombarded [18O]H2O for the production and the application of [18F]F

Rötering, S.; Franke, K.; Zessin, J.; Brust, P.; Füchtner, F.; Fischer, S.; Steinbach, J.


2014

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, C. K.; Deuther-Conrad, W.; Patt, M.; Schildan, A.; Patt, J.; Smits, R.; Hoepping, A.; Schoenknecht, P.; Steinbach, J.; Brust, P.; Sabri, O.


Synthesis and evaluation of a 18F-labeled spirocyclic piperidine derivative as promising σ1 receptor imaging agent

Chen, Y.-Y.; Wang, X.; Zhang, J.-M.; Deuther-Conrad, W.; Zhang, X.-J.; Huang, Y.; Li, Y.; Ye, J.-J.; Cui, M.-C.; Steinbach, J.; Brust, P.; Liu, B.-L.


Novel Cyclopentadienyl Tricarbonyl 99mTc Complexes Containing 1‑Piperonylpiperazine Moiety: Potential Imaging Probes for Sigma‑1 Receptors

Wang, X.; Li, D.; Deuther-Conrad, W.; Lu, J.; Xie, Y.; Jia, B.; Cui, M.; Steinbach, J.; Brust, P.; Liu, B.; Jia, H.


Adenosine activates brown adipose tissue and recruits beige adipocytes via A2A receptors

Gnad, T.; Scheibler, S.; von Kügelgen, I.; Scheele, C.; Kilic, A.; Glöde, A.; Hoffmann, L.; Reverte, L.; Horn, P.; Mutlu, S.; El-Tayeb, A.; Kranz, M.; Deuther-Conrad, W.; Brust, P.; Lidell, M.; Betz, M.; Enerbäck, S.; Schrader, J.; Yegutkin, G.; Mueller, C.; Pfeifer, A.


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

Patt, M.; Becker, G. A.; Grossmann, U.; Habermann, B.; Schildan, A.; Wilke, S.; Deuther-Conrad, W.; Graefe, S.; Fischer, S.; Smits, R.; Wagenknecht, G.; Steinbach, J.; Gertze, H.-J.; Hesse, S.; Schönknecht, P.; Brust, P.; Sabri, O.


Imaging of α7 nicotinic acetylcholine receptors in brain and cerebral vasculature of juvenile pigs with [18F]NS14490

Rötering, S.; Deuther-Conrad, W.; Cumming, P.; Donat, C. K.; Scheunemann, M.; Fischer, S.; Xiong, G.; Steinbach, J.; Peters, D.; Sabri, O.; Bucerius, J.; Brust, P.


Early increase of cannabinoid receptor density after experimental traumatic brain injury in the newborn piglet

Donat, C. K.; Fischer, F.; Walter, B.; Deuther-Conrad, W.; Brodhun, M.; Bauer, R.; Brust, P.

  • Open Access Logo Acta Neurobiologiae Experimentalis 74(2014), 197-210

Distinctive In Vivo Kinetics of the New Sigma1 Receptor Ligands (R)-(+) and (S)-(-)- 18F-Fluspidine in Porcine Brain

Brust, P.; Deuther-Conrad, W.; Becker, G.; Patt, M.; Dont, C. K.; Stittsworth, S.; Fischer, S.; Hiller, A.; Wenzel, B.; Dukic-Stefanovic, S.; Hesse, S.; Steinbach, J.; Wünsch, B.; Lever, S. Z.; Sabri, O.


Asymmetric Synthesis of Spirocyclic 2-Benzopyrans for Positron Emission Tomography of σ1 Receptors in the Brain

Holl, K.; Schepmann, D.; Fischer, S.; Ludwig, F. A.; Hiller, A.; Donat, C. K.; Deuther-Conrad, W.; Brust, P.; Wünsch, B.


Synthesis and biological evaluation of both enantiomers of [18F]flubatine, promising radiotracers with fas 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.


Development of 18F-labeled radiotracers for neuroreceptor imaging with positron emission tomography

Brust, P.; van den Hoff, J.; Steinbach, J.


Hydroxyalkylation with Cyclic Sulfates: Synthesis of Carbazole Derived CB2 Ligands with Increased Polarity

Lueg, C.; Galla, F.; Frehland, B.; Schepmann, D.; Daniliuc, C. G.; Deuther-Conrad, W.; Brust, P.; Wünsch, B.


Automation of the radiosynthesis and purification procedures for [18F]Fluspidine preparation, a new radiotracer for clinical investigations in PET imaging of σ1 receptors in brain.

Maisonial-Besset, A.; Funke, U.; Wenzel, B.; Fischer, S.; Holl, K.; Wünsch, B.; Steinbach, J.; Brust, P.


Molecular Imaging of σ1 Receptors In Vivo: Current Status and Perspectives

Brust, P.; Deuther-Conrad, W.; Lehmkuhl, K.; Jia, H.; Wünsch, B.


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