• Beteiligung an „Cells in Motion“

    • Mitglied der Kommission für Forschung und Karriere
    • Vorstandsmitglied des Graduiertenprogramms CiM-IMPRS
    • Forschungsinteressen: development of novel ligands for various receptors and ion channels, 18F – and fluorescent dye labelled probes
    • Projekt FF-2016-11: Effects of newly generated, peripherally-selective, anti-inflammatory kappa-opioid receptor agonists in the treatment of progressive CNS inflammation and neurodegeneration (Karin Loser, Bernhard Wünsch, Sonja Ständer, Projektlaufzeit: 07/2016 - 10/2018)
    • Projekt FF-2014-03: In vivo intratumoral accumulation of cytotoxic drugs by tumor vascular infarction with retargeted tissue factor tTF-NGR (Wolfgang Berdel, Carsten Höltke, Stefan Wagner, Bernhard Wünsch, Projektlaufzeit: 04/2014 - 03/2015)

  • Publikationen im Forschungsschwerpunkt „Zelldynamik und Bildgebung“

    2020

    Brömmel K, Maskri S, Maisuls I, Konken CP, Rieke M, Petho Z, Strassert CA, Koch O, Schwab A, Wunsch B. Synthesis of Small-Molecule Fluorescent Probes for the In Vitro Imaging of Calcium-Activated Potassium Channel KCa 31. Angew Chem Int Ed Engl 2020;59: 8277-8284. Abstract
    Schepmann D, Neue C, Westphalinger S, Muller C, Bracher F, Lange C, Bednarski P, Almansa C, Friedland K, Rabiger V, Dufer M, Wunsch B. Pharmacological characterization of high-affinity sigma1 receptor ligands with spirocyclic thienopyran and thienofuran scaffold. J Pharm Pharmacol 2020;72: 236-248. Abstract

    2019

    Baumeister S, Schepmann D, Wunsch B. Synthesis and receptor binding of thiophene bioisosteres of potent GluN2B ligands with a benzo[7]annulene-scaffold. MedChemComm. 2019;10: 315-325. Abstract
    Bergkemper M, Kronenberg E, Schepmann D, Ludwig F-A, Brust P, Wunsch B. Structure-Affinity Relationships of Fluorinated Spirocyclic sigma2 Receptor Ligands with an Exocyclic Benzylamino Moiety. ChemMedChem 2019;14: 1392-1402. Abstract
    Borgel F, Galla F, Lehmkuhl K, Schepmann D, Ametamey SM, Wunsch B. Pharmacokinetic properties of enantiomerically pure GluN2B selective NMDA receptor antagonists with 3-benzazepine scaffold. J Pharm Biomed Anal 2019;172: 214-222. Abstract
    Bunse P, Schlepphorst C, Glorius F, Kitamura M, Wunsch B. Short and Atom-Economic Enantioselective Synthesis of the sigma1-Receptor Ligands (S)- and (R)-Fluspidine-Important Tools for Positron Emission Tomography Studies. J Org Chem 2019;84: 13744-13754. Abstract
    Kronenberg E, Weber F, Brune S, Schepmann D, Almansa C, Friedland K, Laurini E, Pricl S, Wunsch B. Synthesis and Structure-Affinity Relationships of Spirocyclic Benzopyrans with Exocyclic Amino Moiety. J Med Chem 2019;62: 4204-4217. Abstract
    Tangherlini G, Kalinin DV, Schepmann D, Che T, Mykicki N, Stander S, Loser K, Wunsch B. Development of Novel Quinoxaline-Based kappa-Opioid Receptor Agonists for the Treatment of Neuroinflammation. J Med Chem 2019;62: 893-907. Abstract
    Temme L, Borgel F, Schepmann D, Robaa D, Sippl W, Daniliuc C, Wunsch B. Impact of hydroxy moieties at the benzo[7]annulene ring system of GluN2B ligands: Design, synthesis and biological evaluation. Bioorg Med Chem 2019;27: 115146. Abstract
    Thum S, Schepmann D, Ayet E, Pujol M, Nieto FR, Ametamey SM, Wunsch B. Tetrahydro-3-benzazepines with fluorinated side chains as NMDA and sigma1 receptor antagonists: Synthesis, receptor affinity, selectivity and antiallodynic activity. Eur J Med Chem 2019;177: 47-62. Abstract
    Thum S, Schepmann D, Reinoso RF, Alvarez I, Ametamey SM, Wunsch B. Synthesis and pharmacological evaluation of fluorinated benzo[7]annulen-7-amines as GluN2B-selective NMDA receptor antagonists. J Labelled Comp Radiopharm 2019;62: 354-379. Abstract
    Wagner M, Schepmann D, Ametamey SM, Wunsch B. Modification of the 4-phenylbutyl side chain of potent 3-benzazepine-based GluN2B receptor antagonists. Bioorg Med Chem 2019;27: 3559-3567. Abstract

    2018

    Bergkemper M, Kronenberg E, Thum S, Borgel F, Daniliuc C, Schepmann D, Nieto FR, Brust P, Reinoso RF, Alvarez I, Wunsch B. Synthesis, Receptor Affinity, and Antiallodynic Activity of Spirocyclic sigma Receptor Ligands with Exocyclic Amino Moiety. J Med Chem 2018;61: 9666-9690. Abstract
    Borgel F, Szermerski M, Schreiber JA, Temme L, Strutz-Seebohm N, Lehmkuhl K, Schepmann D, Ametamey SM, Seebohm G, Schmidt TJ, Wunsch B. Synthesis and Pharmacological Evaluation of Enantiomerically Pure GluN2B Selective NMDA Receptor Antagonists. ChemMedChem 2018;13: 1580-1587. Abstract
    Bunse P, Würthwein E-U, Wünsch B. Synthesis of Substituted 1-Alkylidenephthalanes via Lithium-Promoted 5-exo-dig Cyclization. Eur. J. Org. Chem. 2018: 1806-1812. Abstract
    Butsch V, Borgel F, Galla F, Schwegmann K, Hermann S, Schafers M, Riemann B, Wunsch B, Wagner S. Design, (Radio)Synthesis, and in Vitro and in Vivo Evaluation of Highly Selective and Potent Matrix Metalloproteinase 12 (MMP-12) Inhibitors as Radiotracers for Positron Emission Tomography. J Med Chem 2018;61: 4115-4134. Abstract
    Dey S, Schepmann D, Wunsch B. 2-Methyltetrahydro-3-benzazepin-1-ols - The missing link in SAR of GluN2B selective NMDA receptor antagonists. Bioorg Med Chem 2018;26: 501-508. Abstract
    Fanter L, Schepmann D, Wunsch B. Solid-phase organic synthesis of chiral, non-racemic 1,2,4-trisubstituted 1,4-diazepanes with high sigma1 receptor affinity. Arch Pharm (Weinheim) 2018;351: e1700334. Abstract
    Heimann D, Borgel F, de Vries H, Bachmann K, Rose VE, Frehland B, Schepmann D, Heitman LH, Wunsch B. Optimization of pharmacokinetic properties by modification of a carbazole-based cannabinoid receptor subtype 2 (CB2) ligand. Eur J Med Chem 2018;143: 1436-1447. Abstract
    Heimann D, Borgel F, de Vries H, Patberg M, Jan-Smith E, Frehland B, Schepmann D, Heitman LH, Wunsch B. Optimization of the metabolic stability of a fluorinated cannabinoid receptor subtype 2 (CB2) ligand designed for PET studies. Eur J Med Chem 2018;146: 409-422. Abstract
    Schreiber JA, Müller SL, Westphälinger SE, Schepmann D, Strutz-Seebohm N, Seebohm G, Wünsch B. Systematic variation of the benzoylhydrazine moiety of the GluN2A selective NMDA receptor antagonist TCN-201. Eur J Med Chem 2018;158: 259-269. Abstract
    Szermerski M, Borgel F, Schepmann D, Haider A, Betzel T, Ametamey SM, Wunsch B. Fluorinated GluN2B Receptor Antagonists with a 3-Benzazepine Scaffold Designed for PET Studies. ChemMedChem 2018;13: 1058-1068. Abstract
    Temme L, Frehland B, Schepmann D, Robaa D, Sippl W, Wunsch B. Hydroxymethyl bioisosteres of phenolic GluN2B-selective NMDA receptor antagonists: Design, synthesis and pharmacological evaluation. Eur J Med Chem 2018;144: 672-681. Abstract
    Temme L, Schepmann D, Schreiber JA, Frehland B, Wunsch B. Comparative Pharmacological Study of Common NMDA Receptor Open Channel Blockers Regarding Their Affinity and Functional Activity toward GluN2A and GluN2B NMDA Receptors. ChemMedChem 2018;13: 446-452. Abstract
    Thum S, Schepmann D, Kalinin DV, Ametamey SM, Wunsch B. Replacement of the Benzylpiperidine Moiety with Fluorinated Phenylalkyl Side Chains for the Development of GluN2B Receptor Ligands. ChemMedChem 2018;13: 2522-2529. Abstract
    Torres-Gomez H, Daniliuc C, Schepmann D, Wunsch B. Synthesis of 3-aza[443]propellanes with high sigma1 receptor affinity. Bioorg Med Chem 2018;26: 1705-1712. Abstract
    Zscherp R, Baumeister S, Schepmann D, Wunsch B. Pyridine bioisosteres of potent GluN2B subunit containing NMDA receptor antagonists with benzo[7]annulene scaffold. Eur J Med Chem 2018;157: 397-404. Abstract

    2017

    Asare-Nkansah S, Schepmann D, Wunsch B. Synthesis of conformationally restricted 1,3-dioxanes to analyze the bioactive conformation of 1,3-dioxane-based sigma1 and PCP receptor antagonists. Bioorg Med Chem 2017;25: 2472-2481. Abstract
    Dey S, Temme L, Schreiber JA, Schepmann D, Frehland B, Lehmkuhl K, Strutz-Seebohm N, Seebohm G, Wunsch B. Deconstruction - reconstruction approach to analyze the essential structural elements of tetrahydro-3-benzazepine-based antagonists of GluN2B subunit containing NMDA receptors. Eur J Med Chem 2017;138: 552-564. Abstract
    Fanter L, Muller C, Schepmann D, Bracher F, Wunsch B. Chiral-pool synthesis of 1,2,4-trisubstituted 1,4-diazepanes as novel sigma1 receptor ligands. Bioorg Med Chem 2017;25: 4778-4799. Abstract
    Gawaskar S, Temme L, Schreiber JA, Schepmann D, Bonifazi A, Robaa D, Sippl W, Strutz-Seebohm N, Seebohm G, Wunsch B. Design, Synthesis, Pharmacological Evaluation and Docking Studies of GluN2B-Selective NMDA Receptor Antagonists with a Benzo[7]annulen-7-amine Scaffold. ChemMedChem 2017;12: 1212-1222. Abstract
    Heimann D, Lueg C, de Vries H, Frehland B, Schepmann D, Heitman LH, Wunsch B. Bioisosteric replacement of central 1,2,4-oxadiazole ring of high affinity CB2 ligands by regioisomeric 1,3,4-oxadiazole ring. MedChemComm. 2017;8: 1697-1705. Abstract
    Knappmann I, Lehmkuhl K, Kohler J, Schepmann D, Giera M, Bracher F, Wunsch B. Lipase-catalyzed kinetic resolution as key step in the synthesis of enantiomerically pure sigma ligands with 2-benzopyran structure. Bioorg Med Chem 2017;25: 3384-3395. Abstract
    Kokornaczyk AK, Schepmann D, Yamaguchi J, Itami K, Laurini E, Fermeglia M, Pricl S, Wunsch B. Thiazole-Based sigma1 Receptor Ligands: Diversity by Late-Stage C-H Arylation of Thiazoles, Structure-Affinity and Selectivity Relationships, and Molecular Interactions. ChemMedChem 2017;12: 1070-1080. Abstract
    Kokornaczyk AK, Thum S, Daniliuc CG, Junker A, Wünsch B. Molecular structure of a brominated 2-benzazepinone – a crucial intermediate in the synthesis of novel chemokine CCR2 receptor antagonists. Z. Naturforsch. B 2017;72: 421-424. Abstract
    Muller SL, Schreiber JA, Schepmann D, Strutz-Seebohm N, Seebohm G, Wunsch B. Systematic variation of the benzenesulfonamide part of the GluN2A selective NMDA receptor antagonist TCN-201. Eur J Med Chem 2017;129: 124-134. Abstract
    Ortmeyer CP, Haufe G, Schwegmann K, Hermann S, Schafers M, Borgel F, Wunsch B, Wagner S, Hugenberg V. Synthesis and evaluation of a [18F]BODIPY-labeled caspase-inhibitor. Bioorg Med Chem 2017;25: 2167-2176. Abstract
    Rath S, Schepmann D, Wunsch B. Replacement of benzylic hydroxy group by vinyl or hydroxymethyl moiety at the 3-benzazepine scaffold retaining GluN2B affinity. Bioorg Med Chem 2017;25: 5365-5372. Abstract
    Shuto Y, Thum S, Temme L, Schepmann D, Kitamura M, Wunsch B. Do GluN2B subunit containing NMDA receptors tolerate a fluorine atom in the phenylalkyl side chain?. Medchemcomm 2017;8: 975-981. Abstract
    Thum S, Kokornaczyk AK, Seki T, De Maria M, Ortiz Zacarias NV, de Vries H, Weiss C, Koch M, Schepmann D, Kitamura M, Tschammer N, Heitman LH, Junker A, Wunsch B. Synthesis and biological evaluation of chemokine receptor ligands with 2-benzazepine scaffold. Eur J Med Chem 2017;135: 401-413. Abstract
    Weber F, Brust P, Laurini E, Pricl S, Wunsch B. Fluorinated PET Tracers for Molecular Imaging of sigma1 Receptors in the Central Nervous System. Adv Exp Med Biol 2017;964: 31-48. Abstract
    Wittig C, Schepmann D, Soeberdt M, Daniliuc CG, Wunsch B. Stereoselective synthesis of conformationally restricted KOR agonists based on the 2,5-diazabicyclo[222]octane scaffold. Org Biomol Chem 2017;15: 6520-6540. Abstract

    2016

    Hugenberg V, Hermann S, Galla F, Schafers M, Wunsch B, Kolb HC, Szardenings K, Lebedev A, Walsh JC, Mocharla VP, Gangadharmath UB, Kopka K, Wagner S. Radiolabeled hydroxamate-based matrix metalloproteinase inhibitors: How chemical modifications affect pharmacokinetics and metabolic stability. Nucl Med Biol 2016;43: 424-437. Abstract
    Stucke-Ring J, Ronnacker J, Brand C, Holtke C, Schliemann C, Kessler T, Schmidt LH, Harrach S, Mantke V, Hintelmann H, Hartmann W, Wardelmann E, Lenz G, Wunsch B, Muller-Tidow C, Mesters RM, Schwoppe C, Berdel WE. Combinatorial effects of doxorubicin and retargeted tissue factor by intratumoral entrapment of doxorubicin and proapoptotic increase of tumor vascular infarction. Oncotarget 2016;7: 82458-82472. Abstract
    Weber F, Brune S, Borgel F, Lange C, Korpis K, Bednarski PJ, Laurini E, Fermeglia M, Pricl S, Schepmann D, Wunsch B. Rigidity versus Flexibility: Is This an Issue in sigma1 Receptor Ligand Affinity and Activity?. J Med Chem 2016;59: 5505-5519. Abstract
    Wiese C, Grosse Maestrup E, Galla F, Schepmann D, Hiller A, Fischer S, Ludwig F-A, Deuther-Conrad W, Donat CK, Brust P, Buter L, Karst U, Wunsch B. Comparison of in Silico, Electrochemical, in Vitro and in Vivo Metabolism of a Homologous Series of (Radio)fluorinated σ1 Receptor Ligands Designed for Positron Emission Tomography. ChemMedChem 2016;11: 2445–2458. Abstract

    2015

    Junker A, Kokornaczyk AK, Zweemer AJM, Frehland B, Schepmann D, Yamaguchi J, Itami K, Faust A, Hermann S, Wagner S, Schafers M, Koch M, Weiss C, Heitman LH, Kopka K, Wunsch B. Synthesis, binding affinity and structure-activity relationships of novel, selective and dual targeting CCR2 and CCR5 receptor antagonists. Org Biomol Chem 2015;13: 2407-2422. Abstract
    Quick MP, Frohlich R, Schepmann D, Wunsch B. Asymmetric synthesis of 3-substituted tetrahydro-2-benzazepines. Org Biomol Chem 2015;13: 7265-7281. Abstract
    Strunz AK, Zweemer AJM, Weiss C, Schepmann D, Junker A, Heitman LH, Koch M, Wunsch B. Synthesis and biological evaluation of spirocyclic antagonists of CCR2 (chemokine CC receptor subtype 2). Bioorg Med Chem 2015;23: 4034-4049. Abstract

    2014

    Bourgeois C, Werfel E, Galla F, Lehmkuhl K, Torres-Gomez H, Schepmann D, Kogel B, Christoph T, Strassburger W, Englberger W, Soeberdt M, Huwel S, Galla H-J, Wunsch B. Synthesis and pharmacological evaluation of 5-pyrrolidinylquinoxalines as a novel class of peripherally restricted kappa-opioid receptor agonists. J Med Chem 2014;57: 6845-6860. Abstract
    Brust P, Deuther-Conrad W, Lehmkuhl K, Jia H, Wunsch B. Molecular imaging of sigma1 receptors in vivo: current status and perspectives. Curr Med Chem 2014;21: 35-69. Abstract
    Gawaskar S, Schepmann D, Bonifazi A, Wunsch B. Synthesis, GluN2B affinity and selectivity of benzo[7]annulen-7-amines. Bioorg Med Chem 2014;22: 6638-6646. Abstract
    Hasebein P, Frehland B, Lehmkuhl K, Frohlich R, Schepmann D, Wunsch B. Synthesis and pharmacological evaluation of like- and unlike-configured tetrahydro-2-benzazepines with the alpha-substituted benzyl moiety in the 5-position. Org Biomol Chem 2014;12: 5407-5426. Abstract
    Hasebein P, Frehland B, Schepmann D, Wunsch B. Synthesis, sigma receptor affinity, and pharmacological evaluation of 5-phenylsulfanyl- and 5-benzyl-substituted tetrahydro-2-benzazepines. ChemMedChem 2014;9: 1697-1703. Abstract
    Holl K, Schepmann D, Fischer S, Ludwig F-A, Hiller A, Donat CK, Deuther-Conrad W, Brust P, Wunsch B. Asymmetric Synthesis of Spirocyclic 2-Benzopyrans for Positron Emission Tomography of sigma1 Receptors in the Brain. Pharmaceuticals (Basel) 2014;7: 78-112. Abstract
    Holla K, Schepmann D, Daniliuc CG, Wünsch B. Sharpless asymmetric dihydroxylation as the key step in the enantioselective synthesis of spirocyclic σ1 receptor ligands. Tetrahedron Asymmetry 2014;25: 268–277. Abstract
    Junker A, Kokornaczyk AK, Strunz AK, Wünsch B. Selective and Dual Targeting of CCR2 and CCR5 Receptors: A Current Overview. Chemokines 2014: 1-55. Abstract
    Junker A, Schepmann D, Yamaguchi J, Itami K, Faust A, Kopka K, Wagner S, Wünsch B. Diverse modifications of the 4-methylphenyl moiety of TAK-779 by late-stage Suzuki-Miyaura cross-coupling. Org Biomol Chem 2014;12: 177-186. Abstract
    Miyata K, Moller G, Schepmann D, Wunsch B. Pyridine analogues of spirocyclic sigma(1) receptor ligands. Bioorg Med Chem 2014;22: 4277-4284. Abstract
    Miyata K, Schepmann D, Wunsch B. Synthesis and sigma receptor affinity of regioisomeric spirocyclic furopyridines. Eur J Med Chem 2014;83: 709-716. Abstract
    Schulte A, Saito S, Wünsch B. Stereoselective Synthesis of_cis_,_cis_-Configured Vicinal Triamines: Stereoselective Synthesis of_cis_,_cis_-Configured Vicinal Triamines. Eur J Org Chem 2014;2014: 5749-5756. Abstract
    Weber F, Brune S, Korpis K, Bednarski PJ, Laurini E, Dal Col V, Pricl S, Schepmann D, Wunsch B. Synthesis, pharmacological evaluation, and sigma1 receptor interaction analysis of hydroxyethyl substituted piperazines. J Med Chem 2014;57: 2884-2894. Abstract

    2013

    Brune S, Pricl S, Wunsch B. Structure of the sigma1 receptor and its ligand binding site. J Med Chem 2013;56: 9809-9819. Abstract
    Harel D, Schepmann D, Prinz H, Brun R, Schmidt TJ, Wunsch B. Natural product derived antiprotozoal agents: synthesis, biological evaluation, and structure-activity relationships of novel chromene and chromane derivatives. J Med Chem 2013;56: 7442-7448. Abstract
    Holl K, Falck E, Kohler J, Schepmann D, Humpf H-U, Brust P, Wunsch B. Synthesis, characterization, and metabolism studies of fluspidine enantiomers. ChemMedChem 2013;8: 2047-2056. Abstract
    Junker A, Yamaguchi J, Itami K, Wunsch B. Synthesis of thiophene-based TAK-779 analogues by C-H arylation. J Org Chem 2013;78: 5579-5586. Abstract
    Lueg C, Schepmann D, Gunther R, Brust P, Wunsch B. Development of fluorinated CB(2) receptor agonists for PET studies. Bioorg Med Chem 2013;21: 7481-7498. Abstract