Publications of Institute of Radiopharmaceutical Cancer Research
203 Publications2023
Development of the High-Affinity Carborane-Based Cannabinoid Receptor Type 2 PET Ligand [18F]LUZ5-d8
Ueberham, L.; Gündel, D.; Kellert, M.; Deuther-Conrad, W.; Ludwig, F.-A.; et al. (11 authors)
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Journal of Medicinal Chemistry 66(2023), 5242-5260
DOI: 10.1021/acs.jmedchem.3c00195
Radiofluorination of an anionic, azide-functionalized teroligomer by copper-catalyzed azide-alkyne cycloaddition
Wenzel, B.; Schmid, M.; Teodoro, R.; Moldovan, R.-P.; Lai, T. H.; et al. (11 authors)
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Nanomaterials 13(2023)14, 2095
DOI: 10.3390/nano13142095
Nemacol is a Small Molecule Inhibitor of C. elegans Vesicular Acetylcholine Transporter with Anthelmintic Potential
Harrington, S.; Pyche, J.; Andrew, R. B.; Spalholz, T.; Ryan, K. T.; et al. (15 authors)
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Nature Communications 14(2023), 1816
DOI: 10.1038/s41467-023-37452-6
Imaging of Gαq proteins in mouse and human organs and tissues
Voss, J. H.; Al-Hroub, H.; Gedschold, R.; Dietrich, J.; Gaffal, E.; et al. (13 authors)
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Pharmaceutics 15(2023)1, 57
Online First (2022) DOI: 10.3390/pharmaceutics15010057
Synthesis, Structure–Activity Relationships, Radiofluorination, and Biological Evaluation of [18F]RM365, a Novel Radioligand for Imaging the Human Cannabinoid Receptor Type 2 (CB2R) in the Brain with PET
Teodoro, R.; Gündel, D.; Deuther-Conrad, W.; Toussaint, M.; Wenzel, B.; et al. (9 authors)
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Journal of Medicinal Chemistry 66(2023)20, 13991–14010
DOI: 10.1021/acs.jmedchem.3c01035
2022
Radiosynthesis and preclinical evaluation of an 18F-labeled tri-azolopyridopyrazine-based inhibitor for neuroimaging of the phosphodiesterase 2A (PDE2A)
Wenzel, B.; Fritzsche, S. R.; Toussaint, M.; Briel, D.; Kopka, K.; et al. (8 authors)
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Pharmaceuticals 15(2022)10, 1272
DOI: 10.3390/ph15101272
Synthesis and characterization of the two enantiomers of a chiral sigma-1 receptor radioligand: (S)-(+)- and (R)-(-)-[18F]FBFP
Wang, T.; Zhang, Y.; Zhang, X.; Chen, L.; Zheng, M.-Q.; et al. (10 authors)
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Chinese Chemical Letters 33(2022)7, 3543-3548
DOI: 10.1016/j.cclet.2022.03.099
Amphiphilic Anionic Oligomer-Stabilized Calcium Phosphate Nanoparticles with Prospects in siRNA Delivery via Convection-Enhanced Delivery
Mitrach, F.; Schmid, M.; Toussaint, M.; Dukic-Stefanovic, S.; Deuther-Conrad, W.; et al. (12 authors)
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Pharmaceutics 14(2022)2, 326
DOI: 10.3390/pharmaceutics14020326
Development and Biological Evaluation of the First Highly Potent and Specific Benzamide-Based Radiotracer [¹⁸F]BA3 for Imaging of Histone Deacetylases 1 and 2 in Brain
Clauß, O.; Schäker-Hübner, L.; Wenzel, B.; Toussaint, M.; Deuther-Conrad, W.; et al. (13 authors)
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Pharmaceuticals 15(2022)3, 324
DOI: 10.3390/ph15030324
Structure-Based Design, Optimization and Development of [18F]LU13, a novel radioligand for CB2R Imaging in the Brain with PET
Gündel, D.; Deuther-Conrad, W.; Ueberham, L.; Kaur, S.; Otikova, E.; et al. (14 authors)
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Journal of Medicinal Chemistry 65(2022)13, 9034-9049
DOI: 10.1021/acs.jmedchem.2c00256
Automated radiosynthesis of the adenosine A2A receptor-targeting radiotracer [18F]FLUDA
Lai, T. H.; Wenzel, B.; Moldovan, R.-P.; Brust, P.; Kopka, K.; et al. (6 authors)
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Journal of Labelled Compounds and Radiopharmaceuticals 65(2022), 162-166
DOI: 10.1002/jlcr.3970
Non-invasive assessment of locally overexpressed human adenosine 2A receptors in the heart of transgenic mice
Gündel, D.; Lai, T. H.; Dukic-Stefanovic, S.; Teodoro, R.; Deuther-Conrad, W.; et al. (13 authors)
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International Journal of Molecular Sciences 23(2022)3, 1025
DOI: 10.3390/ijms23031025
Discovery and development of brain-penetrant 18F-labeled radioligands for neuroimaging of the sigma-2 receptors
Zhang, Y.; Wang, T.; Zhang, X.; Deuther-Conrad, W.; Fu, H.; et al. (10 authors)
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Acta Pharmaceutica Sinica B 12(2022)3, 1406-1415
Online First (2021) DOI: 10.1016/j.apsb.2021.08.029
2021
Leptin counteracts hypothermia in hypothyroidism through its pyrexic effects and by stabilizing serum thyroid hormone levels
Weiner, J.; Roth, L.; Kranz, M.; Brust, P.; Boelen, A.; et al. (13 authors)
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Molecular Metabolism 54(2021), 101348
DOI: 10.1016/j.molmet.2021.101348
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.; et al. (16 authors)
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Frontiers in Neurology 12(2021), 642604
DOI: 10.3389/fneur.2021.642604
Development of [18F]LU14 for PET Imaging of Cannabinoid Receptor Type 2 in the Brain
Teodoro, R.; Gündel, D.; Ueberham, L.; Toussaint, M.; Bormans, G.; et al. (8 authors)
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International Journal of Molecular Sciences 22(2021)15, 8051
DOI: 10.3390/ijms22158051
Development of fluorinated and methoxylated benzothiazole derivatives as highly potent and selective cannabinoid CB2 receptor ligands
Aly, M. W.; Ludwig, F.-A.; Deuther-Conrad, W.; Brust, P.; Abadi, A. H.; et al. (7 authors)
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Bioorganic Chemistry 114(2021), 105191
DOI: 10.1016/j.bioorg.2021.105191
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.; et al. (10 authors)
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Pharmaceuticals 14(2021), 485
DOI: 10.3390/ph14050485
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.; et al. (10 authors)
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International Journal of Molecular Sciences 22(2021)11, 5447
DOI: 10.3390/ijms22115447
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.
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International Journal of Molecular Sciences 22(2021)8, 3832
DOI: 10.3390/ijms22083832
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.; et al. (8 authors)
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Pharmaceuticals 14(2021), 259
DOI: 10.3390/ph14030259
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.; et al. (13 authors)
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International Journal of Molecular Sciences 22(2021)4, 1645
DOI: 10.3390/ijms22041645
ISSN: 1422-0067
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.; et al. (8 authors)
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International Journal of Molecular Sciences 22(2021)3, 1182
DOI: 10.3390/ijms22031182
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.; et al. (11 authors)
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International Journal of Molecular Sciences 22(2021)5, 2285
DOI: 10.3390/ijms22052285
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.; et al. (14 authors)
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European Journal of Nuclear Medicine and Molecular Imaging 48(2021), 2727-2736
DOI: 10.1007/s00259-020-05164-4
In vitro and in vivo evaluation of fluorinated indanone derivatives as potential positron emission tomography agents for the imaging of monoamine oxidase B in the brain
Dukic-Stefanovic, S.; Lai, T. H.; Toussaint, M.; Clauß, O.; Jevtić, I. I.; et al. (13 authors)
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Bioorganic & Medicinal Chemistry Letters 48(2021), 128254
DOI: 10.1016/j.bmcl.2021.128254
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.; et al. (24 authors)
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European Journal of Nuclear Medicine and Molecular Imaging 48(2021), 1103-1115
Online First (2020) DOI: 10.1007/s00259-020-05030-3
(+)-[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.; et al. (21 authors)
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European Journal of Nuclear Medicine and Molecular Imaging 48(2021), 731-746
Online First (2020) DOI: 10.1007/s00259-020-05029-w
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.; et al. (6 authors)
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International Journal of Molecular Sciences 21(2020)17, 6189
DOI: 10.3390/ijms21176189
Adenosine/A2B Receptor Signaling Ameliorates the Effects of Aging and Counteracts Obesity
Gnad, T.; Navarro, G.; Lahesmaa, M.; Reverte-Salisa, L.; Copperi, F.; et al. (31 authors)
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Cell Metabolism 32(2020), 56-70
DOI: 10.1016/j.cmet.2020.06.006
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.; et al. (11 authors)
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Molecules 25(2020)9, 2170
DOI: 10.3390/molecules25092170
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.; et al. (12 authors)
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Bioorganic & Medicinal Chemistry 28(2020)14, 115560
DOI: 10.1016/j.bmc.2020.115560
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.; et al. (13 authors)
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International Journal of Molecular Sciences 21(2020), 3197
DOI: 10.3390/ijms21093197
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.; et al. (13 authors)
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Molecules 25(2020)10, 2309
DOI: 10.3390/molecules25102309
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.; et al. (13 authors)
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Molecules 25(2020)9, 2024
DOI: 10.3390/molecules25092024
The sigma-1 receptor: potential role in the modulation of cellular radiation sensitivity
Belter, B.; Deuther-Conrad, W.; Hofheinz, F.; Bachmann, M.; Brust, P.; et al. (6 authors)
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Journal of Cellular Biotechnology 6(2020), 13-21
DOI: 10.3233/JCB-209007
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.; et al. (8 authors)
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Molecules 25(2020)21, 4941
DOI: 10.3390/molecules25214941
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.; et al. (13 authors)
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Molecules 25(2020)7, 1633
DOI: 10.3390/molecules25071633
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.; et al. (10 authors)
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Molecules 24(2019)22, 4149
DOI: 10.3390/molecules24224149
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.
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Scientific Reports 9(2019), 18890
DOI: 10.1038/s41598-019-55354-w
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.; et al. (6 authors)
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ChemMedChem 14(2019), 1392-1402
DOI: 10.1002/cmdc.201900284
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.; et al. (9 authors)
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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.
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Molecules 24(2019)15, 2791
DOI: 10.3390/molecules24152791
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.; et al. (17 authors)
- 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.; et al. (15 authors)
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Frontiers in Pharmacology 10(2019), 534
DOI: 10.3389/fphar.2019.00534
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.; et al. (14 authors)
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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.; et al. (10 authors)
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Bioorganic Chemistry 86(2019), 346-362
DOI: 10.1016/j.bioorg.2019.01.037
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.; et al. (9 authors)
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European Journal of Medicinal Chemistry (2019), 142-159
DOI: 10.1016/j.ejmech.2019.01.006
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.; et al. (11 authors)
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Journal of Medicinal Chemistry 61(2018), 9666-9690
DOI: 10.1021/acs.jmedchem.8b01183
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.
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Forecasting 1(2018), 135-156
DOI: 10.3390/forecast1010010
ISSN: 2571-9394
Cognitive correlates of α4β2 nicotinic acetylcholine receptors in mild Alzheimer's dementia
Sabri, O.; Meyer, P. M.; Gräf, S.; Hesse, S.; Wilke, S.; et al. (21 authors)
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Brain 141(2018)6, 1840-1854
DOI: 10.1093/brain/awy099
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.; et al. (13 authors)
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Bioorganic & Medicinal Chemistry 26(2018), 4650-4663
DOI: 10.1016/j.bmc.2018.07.045
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.; et al. (6 authors)
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Bioorganic & Medicinal Chemistry Letters 28(2018), 1471-1475
DOI: 10.1016/j.bmcl.2018.03.081
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.; et al. (9 authors)
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Molecules 23(2018)1, 464
DOI: 10.3390/molecules23020464
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.; et al. (11 authors)
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Molecules 23(2018)3, 556
DOI: 10.3390/molecules23030556
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.; et al. (14 authors)
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Molecules 23(2018)3, 702
DOI: 10.3390/molecules23030702
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.; et al. (21 authors)
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Translational Psychiatry 7(2017)e1120, 1-13
DOI: 10.1038/tp.2017.80
PET Imaging Evaluation of Four sigma1 Radiotracers in Nonhuman Primates
Baum, E.; Cai, Z.; Bois, F.; Holden, D.; Lin, S.-F.; et al. (16 authors)
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Journal of Nuclear Medicine 58(2017)6, 982
DOI: 10.2967/jnumed.116.188052
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.; et al. (12 authors)
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Journal of Medicinal Chemistry 60(2017), 4161-4172
DOI: 10.1021/acs.jmedchem.6b01723
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.; et al. (11 authors)
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Bioorganic & Medicinal Chemistry 25(2017), 3792-3802
DOI: 10.1016/j.bmc.2017.05.019
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.; et al. (8 authors)
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Bioorganic & Medicinal Chemistry 25(2017)19, 5095-5106
DOI: 10.1016/j.bmc.2017.01.041
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.; et al. (8 authors)
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Applied Radiation and Isotopes 124(2017), 106-113
DOI: 10.1016/j.apradiso.2017.03.015
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.; et al. (6 authors)
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Bioorganic & Medicinal Chemistry 25(2017)19, 5107-5113
DOI: 10.1016/j.bmc.2017.03.028
Development of highly affine and selective fluorinated cannabinoid receptor type 2 ligands
Moldovan, R.-P.; Hausmann, K.; Deuther-Conrad, W.; Brust, P.
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ACS Medicinal Chemistry Letters (2017), 566-571
DOI: 10.1021/acsmedchemlett.7b00129
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.; et al. (9 authors)
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International Journal of Molecular Sciences 18(2017)4, 768
DOI: 10.3390/ijms18040768
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.; et al. (17 authors)
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European Journal of Nuclear Medicine and Molecular Imaging 44(2017)6, 1042-1050
DOI: 10.1007/s00259-017-3621-8
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.; et al. (14 authors)
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Frontiers in Neuroscience 10(2017), 620
Online First (2016) DOI: 10.3389/fnins.2016.00620
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.; et al. (8 authors)
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European Journal of Medicinal Chemistry 136(2017), 548-560
DOI: 10.1016/j.ejmech.2017.03.091
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.
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PLOS ONE 12(2017)7, e0179919.
DOI: 10.1371/journal.pone.0179919
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.; et al. (11 authors)
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Journal of Nuclear Medicine 58(2017)7, 1100-1103
DOI: 10.2967/jnumed.116.186460
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.
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Molecules 22(2017)1, 77
DOI: 10.3390/molecules22010077
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.; et al. (17 authors)
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Cell Metabolism 25(2017)2, 335-344
Online First (2016) DOI: 10.1016/j.cmet.2016.12.006
Radiosynthesis and biological evaluation of the new PDE10A radioligand [18F]AQ28A
Wagner, S.; Teodoro, R.; Deuther-Conrad, W.; Kranz, M.; Scheunemann, M.; et al. (11 authors)
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Journal of Labelled Compounds and Radiopharmaceuticals 60(2017)1, 36-48
Online First (2016) DOI: 10.1002/jlcr.3471
2016
Targetting microglia activation in schizophrenia by minocycline treatment
Mattei, D.; Ivanov, A.; Ferrai, G.; Jordan, P.; Guneykaya, D.; et al. (16 authors)
- 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.; et al. (13 authors)
-
Molecules 21(2016), 1164
DOI: 10.3390/molecules21091164
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.; et al. (10 authors)
-
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Synthesis and biological evaluation of a radioiodinated spiropiperidine ligand as a potential σ1 receptor imaging agent
Chen, R.-Q.; Li, Y.; Zhang, Q.-Y.; Jia, H.-M.; Deuther-Conrad, W.; et al. (10 authors)
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Journal of Labelled Compounds and Radiopharmaceuticals 53(2010), 569-574
DOI: 10.1002/jlcr.1777
Design, Synthesis and in Vitro Biological Evaluation of Reference Compounds of 123I and 99Tcm Labeled Indole Radiotracers for σ2 Receptor Imaging
Li, Y.; Jia, H.-M.; Deuther-Conrad, W.; Brust, P.; Steinbach, J.; et al. (6 authors)
- Journal of Nuclear and Radiochemistry 32(2010)2, 132-138
Effects of lateral fluid percussion injury on cholinergic markers in the newborn piglet brain
Donat, C. K.; Walter, B.; Kayser, T.; Deuther-Conrad, W.; Schliebs, R.; et al. (9 authors)
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International Journal of Developmental Neuroscience 28(2010), 31-38
DOI: 10.1016/j.ijdevneu.2009.10.001
Novel Indole Derivatives as Potential Imaging Agents for Alzheimers Disease
Yu, L.; Scheunemann, M.; Deuther-Conrad, W.; Hiller, A.; Fischer, S.; et al. (11 authors)
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Bulletin of the Korean Chemical Society 31(2010)1, 177-180
DOI: 10.5012/bkcs.2010.31.01.177
Enantioseparation of vesamicol and novel vesamicol analogs by high-performance liquid chromatography on different chiral stationary phases
Wenzel, B.; Fischer, S.; Brust, P.; Steinbach, J.
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Journal of Chromatography A 1217(2010), 3855-3862
DOI: 10.1016/j.chroma.2010.04.018
2009
Molecular imaging of α7 nicotinic acetylcholine receptors: design and evaluation of the potent radioligand [18F]NS10743
Deuther-Conrad, W.; Fischer, S.; Hiller, A.; Ostergaard Nielsen, E.; Brunicardi Timmermann, D.; et al. (9 authors)
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European Journal of Nuclear Medicine and Molecular Imaging 36(2009), 791-800
DOI: 10.1007/s00259-008-1031-7
2008
3-(4-(6-Fluoroalkoxy-3,4-dihydroisoquinolin-2(1H)-yl)cyclohexyl)-1H-indole-5-carbonitriles for SERT imaging: chemical synthesis, evaluation in vitro and radiofluorination
Funke, U.; Fischer, S.; Hiller, A.; Scheunemann, M.; Deuther-Conrad, W.; et al. (7 authors)
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Bioorganic & Medicinal Chemistry Letters 18(2008), 4727-4730
DOI: 10.1016/j.bmcl.2008.06.077
Synthesis and in vitro evaluation of new diphenyl ether derivatives as serotonin transporter ligands
Guo, Y.; Chen, X.; Jia, H.; Deuther-Conrad, W.; Brust, P.; et al. (8 authors)
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Science in China Series B: Chemistry 51(2008)5, 457-463
DOI: 10.1007/s11426-008-0007-6
Radiosynthesis of novel 18F-labelled derivatives of indiplon as potential GABAA receptor imaging tracers for PET
Fischer, S.; Hiller, A.; Scheunemann, M.; Deuther-Conrad, W.; Hoepping, A.; et al. (9 authors)
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Journal of Labelled Compounds and Radiopharmaceuticals 51(2008), 123-131
DOI: 10.1002/jlcr.1473
2006
[11C]SMe-ADAM, an imaging agent for the brain serotonin transporter: Synthesis, pharmacological characterization and microPET studies in rats
Zessin, J.; Deuther-Conrad, W.; Kretzschmar, M.; Wüst, F.; Pawelke, B.; et al. (8 authors)
- Nuclear Medicine and Biology 33(2006)1, 53-63
2005
Effect of Moderate Hypercapnic Hypoxia on Cerebral Dopaminergic Activity and Brain O2 Uptake in Intrauterine GrowthRestricted Newborn Piglets
Bauer, R.; Walter, B.; Vorwieger, G.; Fritz, A.; Füchtner, F.; et al. (7 authors)
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Pediatric Research 57(2005)3, 363-370
DOI: 10.1203/01.PDR.0000150800.19956.F0
2004
The Influx of Neutral Amino Acids into the Porcine Brain During Development: A Positron Emission Tomography Study
Brust, P.; Vorwieger, G.; Walter, B.; Füchtner, F.; Stark, H.; et al. (8 authors)
- Developmental Brain Research 152(2004), 241-253
Developmental changes in the activity of aromatic amino acid decarboxylase and catechol-O-methyl transferase in pigs: a positron emission tomography study
Brust, P.; Walter, B.; Hinz, R.; Füchtner, F.; Müller, M.; et al. (7 authors)
- Neuroscience Letters, 364(2004)3, 159-163
Age-dependent effects of severe traumatic brain injury on cerebral dopaminergic activity in newborn and juvenile pigs
Walter, B.; Brust, P.; Füchtner, F.; Müller, M.; Hinz, R.; et al. (9 authors)
- Journal of Neurotrauma 21(2004)8, 1076-1089
2003
Impact of asymmetric intrauterine growth restriction on organ function in newborn piglets
Bauer, R.; Walter, B.; Brust, P.; Füchtner, F.; Zwiener, U.
- European Journal of Obstetrics and Gynecology and Reproductive Biology 110 (2003) S40-S49
S-[18F]fluoromethyl-(+)-McN5652, a PET Tracer for the Serotonin Transporter: Evaluation in Rats
Marjamäki, P.; Zessin, J.; Eskola, O.; Grönroos, T.; Haaparanta, M.; et al. (11 authors)
- Synapse (2003) 47: 45-53
In vivo Measurement of the Serotonin Transporter with (S)-([18F]fluoromenthyl)-(+)-McN5652
Brust, P.; Hinz, R.; Kuwabara, H.; Hesse, S.; Zessin, J.; et al. (10 authors)
- Neuropsychopharmacology (2003) 28, 2010-2019
Positron Emission Tomography Imaging of the Serotonin Transporter in the Pig Brain Using [11C](+)-McN5652 and S-([18F]fluoromethyl)-(+)-McN5652
Brust, P.; Zessin, J.; Kuwabara, H.; Pawelke, B.; Kretzschmar, M.; et al. (11 authors)
- Synapse (2003) 47: 143-151
Autoradiographic analyses of 5-HT1A and 5-HT2A receptors after social isolation in mice
Schiller, L.; Jähkel, M.; Kretzschmar, M.; Brust, P.; Oehler, J.
- Brain Research 980 (2003) 169-178
Autoradiographic imaging of the serotonin ransporter in the brain of rats and pigs using S-([18F]Fluoromethyl)-(+)-McN5652
Kretzschmar, M.; Brust, P.; Zessin, J.; Cumming, P.; Bergmann, R.; et al. (6 authors)
- European Neuropsychopharmacology 13 (2003) 387-397
2002
Effect of hypoxia/hypercapnia on metabolism of 6-[18F]fluoro-L-DOPA in newborn piglets
Bauer, R.; Brust, P.; Walter, B.; Vorwieger, G.; Bergmann, R.; et al. (12 authors)
- Brain Research 934 (2002) 22-33
Tc and Re chelates of 8alpha-amino-6-methyl-ergoline: synthesis and affinity to the dopamine D2 receptor
Spies, H.; Noll, B.; Noll, S.; Findeisen, M.; Brust, P.; et al. (7 authors)
- Bioorganic and Medicinal Chemistry 10 (2002) 3523-3528
Distribution of estrone sulfatase in rat brain determined by in vitro autoradiography with 16alpha-[18F]fluoroestradiol-3,17beta-disulfamate
Rodig, H.; Brust, P.; Römer, J.; Kasch, H.; Bergmann, R.; et al. (8 authors)
- Applied Radiation and Isotopes 56 (2002) 773-780
Distribution of 16alpha-[18F]fluoro-estradiol-3,17beta-disulfamate (FESDS) in rats, tumour-bearing mice and piglets
Brust, P.; Rodig, H.; Römer, J.; Kasch, H.; Bergmann, R.; et al. (10 authors)
- Applied Radiation and Isotopes 57 (2002) 687-695
Synthesis , biological and autoradiographic evaluation of a novel Tc-99m radioligand derived from WAY 100635 with high-affinity for the 5-HT1A receptor and the alpha1-adrenergic receptor
Heimbold, I.; Drews, A.; Kretzschmar, M.; Varnäs, K.; Hall, H.; et al. (12 authors)
- Nuclear Medicine and Biology 29 (2002) 375-387
2001
Comparison of [18F]FHPG and [124/125I]FIAU for imaging herpes simplex virus type 1 tymidine kinase gene expression
Brust, P.; Haubner, R.; Friedrich, A.; Scheunemann, M.; Anton, M.; et al. (14 authors)
- European Journal of Nuclear Medicine Vol.28, No. 6, (2001) 721-729
Synthesis of S-([18F]fluoromethyl)-(+)-McN5652 as a potential PET radioligand for the serotonin transporter
Zessin, J.; Eskola, O.; Brust, P.; Bergman, J.; Steinbach, J.; et al. (8 authors)
- Nuclear Medicine and Biology 28 (2001) 857-863
Quantitative Radioluminography of Serotonin Uptake Sites in the Porcine Brain
Cumming, P.; Kretzschmar, M.; Brust, P.; Smith, D. F.
- Synapse 39 (2001) 351-355
Intrauterine growth restriction induces up-regulation of cerebral aromatic amino acid decarboxylase activity in newborn piglets: [18F]fluorodopa positron-emission-tomographic study
Bauer, R.; Walter, B.; Vorwieger, G.; Bergmann, R.; Füchtner, F.; et al. (6 authors)
- Pediatric Research 49 (2001) 474-480
Reactivity of 99mTc(V) "3+1" mixed-ligand complexes towards glutathione
Gupta, A.; Seifert, S.; Syhre, R.; Scheunemann, M.; Brust, P.; et al. (6 authors)
- Radiochimica Acta 89 (2001) 43-49
2000
Assessment of the in vitro and in vivo properties of a 99mTc-labeled inhibitor of the multidrug resistant gene product P-glycoprotein.
Bergmann, R.; Brust, P.; Scheunemann, M.; Pietzsch, H.-J.; Seifert, S.; et al. (7 authors)
- Nucl. Med. Biol. 27 (2000) 135-141
Relation between brain tissue pO2 and dopamine synthesis of basal ganglia - A 18FDOPA-PET study in newborn piglets
Bauer, R.; Brust, P.; Walter, B.; Vorwieger, G.; Bergmann, R.; et al. (11 authors)
- J. Perinat. Med. 28 (2000) 54-60
Functional expression of the serotonin transporter in immortalized rat brain microvessel endothelial cells
Brust, P.; Friedrich, A.; Krizbai, I. A.; Bergmann, R.; Roux, F.; et al. (7 authors)
- J.Neurochem. 74, (2000) 1241-1248
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Journal of Cerebral Blood Flow and Metabolism, Vol. 19 (Suppl.1), 245
DOI: 10.1046/j.1471-4159.2000.741241.x
1999
Upregulation of the Aromatic Amino Acid Decarboxylase under Neonatal Asphyxia
Brust, P.; Bauer, R.; Vorieger, G.; Walter, B.; Bergmann, R.; et al. (9 authors)
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Neurobiology of Disease 6, (1999) 131-139
DOI: 10.1006/nbdi.1998.0232
Regional distribution of cerebral blood volume and cerebral blood flow in newborn piglets - effect of hypoxia / hypercapnia
Bauer, R.; Bergmann, R.; Walter, B.; Brust, P.; Zwiener, U.; et al. (6 authors)
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Developmental Brain Research 112 (1999) 89-98
DOI: 10.1016/S0165-3806(98)00167-9
Synthesis and preliminary pharmacological investigations of 1-(1,2-dihydro-2-acenaphthylenyl)piperazine derivatives as potential atypical antipsychotic agents in mice
Srinivas, P.; Subramanian, A. R.; Brust, P.; Raghavan, S. A. V.; Rangisetty, J. B.; et al. (9 authors)
- IL FARMACO 54 (1999) 567-572
Synthesis and Autoradiographical Evaluation of a Novel High-Affinity Tc-99m Ligand for the 5-HT2A Receptor
Pietzsch, H.-J.; Scheunemann, M.; Kretzschmar, M.; Elz, S.; Pertz, H. H.; et al. (10 authors)
- Nuclear Medicine and Biology, 26 (1999) 865-875
Synthesis and preliminary binding affinities of 1(1,2-dihydro-2-acenaphthylenyl)piperazine - a new arylpiperazine
Srinivas, P.; Brust, P.; Subramanian, A. R.; Raghavan, S. A. V.; Rangisetty, J. B.; et al. (7 authors)
- Pharmaceutica Acta Helvetiae 74 (1999) 73-73
Efficient Synthesis of Enantiomerically Pure Thioester Precursors of [11C] MCN-5652 from Racemic MCN-5652
Zessin, J.; Gucker, P.; Ametamey, S. M.; Steinbach, J.; Brust, P.; et al. (8 authors)
- J. Labelled Cpd. Radiopharm. 42 (1999) 1301-1312
Radioligands for the Study of the 5-HT Transporter in Vivo
Brust, P.; Scheffel, U.; Szabo, Z.
- IDrugs 1999 Vol 2 No 2 , Review Radioligands 129-145
1998
TROTEC-1 a new high affinity ligand for Labeling of the dopamine transporter
Hoepping, A.; Reisgys, M.; Brust, P.; Seifert, S.; Spies, H.; et al. (7 authors)
- Journal of Medicinal Chemistry, 41(23) (1998) 4429-4432
Differentiation Between Specific and Nonspecific Effects Related to P-Glycoprotein Inhibition in Immortalized Rat Brain Endothelial Cells
Bergmann, R.; Brust, P.; Johannsen, B.
- International Journal of Clinical Pharmacology and Therapeutics, Vol. 36, No. 1, 1998 (46-49)
Simultaneous Measurement of 18F-FDOPA Metabolism and Cerebral Blood Flow in Newborn Piglets
Brust, P.; Bauer, R.; Walter, B.; Bergmann, R.; Füchtner, F.; et al. (9 authors)
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Int. J. Devl. Neuroscience, Vol. 16, No. 5, pp 353-364, 1998
DOI: 10.1016/S0736-5748(98)00017-3
Novel Rhenium Complexes Derived from ALPHA-Tropanol as Potential Ligands for the Dopamin Transporter
Hoepping, A.; Brust, P.; Berger, R.; Leibnitz, P.; Spies, H.; et al. (8 authors)
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Bioorganic & Medicinal Chemistry 6 (1998) 1663-1672
DOI: 10.1016/S0968-0896(98)00144-8
1997
Different response of cerebral and non-cerebral endothelial cells to cytotoxic hypoxia
Ahlemeyer, B.; Brust, P.; Johannsen, B.
- Neurochem. Int. 31 (1997) 39-44
Structural modification of receptor binding 99m-Tc complexes in order to improve brain uptake
Johannsen, B.; Berger, R.; Brust, P.; Pietzsch, H.-J.; Scheunemann, M.; et al. (8 authors)
- European Journal of Nuclear Medicine 24 (1997) 3 pp. 316-319
1996
High-affinity binding of [3H]paroxetine to caudate nucleus and microvessels from porcine brain
Brust, P.; Bergmann, R.; Johannsen, B.
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NeuroReport 7 (1996) pp. 1405-1408
DOI: 10.1097/00001756-199605310-00016
Technetium(V) and Rhenium(V) Complexes for 5-HT2A Serotonin Receptor Binding: Structure-Affinity Considerations
Johannsen, B.; Scheunemann, M.; Spies, H.; Brust, P.; Wober, J.; et al. (7 authors)
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Journal of Nuclear Medicine and Biology 23 (1996) 429-438
DOI: 10.1016/0969-8051(96)00015-7
1995
Specific binding of (3H)imipramine indicates the presence of a specific serotonin transport system on endothelial cells of porcine brain
Brust, P.; Bergmann, R.; Johannsen, B.
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Neuroscience Letters 194 (1995) 21-24
DOI: 10.1016/0304-3940(95)11709-6
Evaluation of Radioselenium Labeled Selenomethionine, a Potential Tracer for Brain Protein Synthesis by PET
Bergmann, R.; Brust, P.; Kampf, G.; Coenen, H. H.; Stöcklin, G.
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J. Nucl. Med. Biol. 22 (1995) 475-481
DOI: 10.1016/0969-8051(94)00123-2
1994
Characterization of serotonin uptake sites on the blood brain barrier
Brust, P.; Bergmann, R.
- Journal of Neurochemistry 63 (1994) (Suppl. 1) S13C
Compartmental analysis of blood brain transfer and protein incorporation of L-[75Se]seleno methionine in rat brain
Bergmann, R.; Brust, P.; Coenen, H. H.; Stöcklin, G.
- Journal of Neurochemistry 63 (1994) (Suppl. 1) S78C
Developmental changes of enzymes involved in peptide degradation in isolated rat brain microvessels
Brust, P.; Bech, A.; Kretzschmar, R.; Bergmann, R.
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Peptides 15 (1994) 6 pp. 1085-1088
DOI: 10.1016/0196-9781(94)90074-4