Search Results - "Schepmann, Dirk"

Deconstruction - Reconstruction: Analysis of the Crucial Structural Elements of GluN2B-Selective, Negative Allosteric NMDA Receptor Modulators with 3-Benzazepine Scaffold by Ritter, Nadine, Korff, Marvin, Markus, Alexander, Schepmann, Dirk, Seebohm, Guiscard, Schreiber, Julian A, Wünsch, Bernhard

“…The NMDA receptor plays a key role in the pathogenesis of neurodegenerative disorders including Alzheimer's and Huntington's disease, as well as depression and…”
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Relationships between the structure of spiro[[2]benzopyran-1,1′-cyclohexan]-4′-amines and their σ1 receptor affinity and selectivity by Kronenberg, Elisabeth, Schepmann, Dirk, Wünsch, Bernhard

“…A set of 31 secondary and tertiary amines of type 5 was synthesized by reductive amination of ketones 6 and 22–24 with amines and NaBH(OAc)3. Usually,…”
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Improvement of σ1 receptor affinity by late-stage C–H-bond arylation of spirocyclic lactones by Meyer, Christina, Neue, Benedikt, Schepmann, Dirk, Yanagisawa, Shuichi, Yamaguchi, Junichiro, Würthwein, Ernst-Ulrich, Itami, Kenichiro, Wünsch, Bernhard

“…Selective α- and β-arylation of complex thiophene annulated lactones with iodoarenes in the last step of the synthesis allows fine tuning of σ1 receptor…”
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Natural Product Derived Antiprotozoal Agents: Synthesis, Biological Evaluation, and Structure–Activity Relationships of Novel Chromene and Chromane Derivatives by Harel, Dipak, Schepmann, Dirk, Prinz, Helge, Brun, Reto, Schmidt, Thomas J, Wünsch, Bernhard

“…Various natural products with the chromane and chromene scaffold exhibit high antiprotozoal activity. The natural product encecalin (7) served as key…”
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Synthesis, GluN2B affinity and selectivity of benzo[7]annulen-7-amines by Gawaskar, Sandeep, Schepmann, Dirk, Bonifazi, Alessandro, Wünsch, Bernhard

“…[Display omitted] Due to their beneficial side effect profile, NMDA receptor antagonists interacting selectively with the allosteric ifenprodil binding site of…”
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Enantiomerically Pure 1,3-Dioxanes as Highly Selective NMDA and σ1 Receptor Ligands by Köhler, Jens, Bergander, Klaus, Fabian, Jörg, Schepmann, Dirk, Wünsch, Bernhard

“…We synthesized and investigated the NMDA and σ1 receptor affinity of enantiomerically pure 2-(2-phenyl-1,3-dioxan-4-yl)ethanamines 17–26. The primary amines…”
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Propellanes as Rigid Scaffolds for the Stereodefined Attachment of σ-Pharmacophoric Structural Elements to Achieve σ Affinity by Torres-Gómez, Héctor, Daniliuc, Constantin, Schepmann, Dirk, Laurini, Erik, Pricl, Sabrina, Wünsch, Bernhard

“…Following the concept of conformationally restriction of ligands to achieve high receptor affinity, we exploited the propellane system as rigid scaffold…”
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Setup and Validation of a Reliable Docking Protocol for the Development of Neuroprotective Agents by Targeting the Sigma-1 Receptor (S1R) by Rossino, Giacomo, Rui, Marta, Pozzetti, Luca, Schepmann, Dirk, Wünsch, Bernhard, Zampieri, Daniele, Pellavio, Giorgia, Laforenza, Umberto, Rinaldi, Silvia, Colombo, Giorgio, Morelli, Laura, Linciano, Pasquale, Rossi, Daniela, Collina, Simona

“…Sigma-1 receptor (S1R) is a promising molecular target for the development of novel effective therapies against neurodegenerative diseases. To speed up the…”
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Design, Radiosynthesis and Preliminary Biological Evaluation in Mice of a Brain-Penetrant 18F-Labelled σ2 Receptor Ligand by Moldovan, Rareş-Petru, Gündel, Daniel, Teodoro, Rodrigo, Ludwig, Friedrich-Alexander, Fischer, Steffen, Toussaint, Magali, Schepmann, Dirk, Wünsch, Bernhard, Brust, Peter, Deuther-Conrad, Winnie

“…The σ2 receptor (transmembrane protein 97), which is involved in cholesterol homeostasis, is of high relevance for neoplastic processes. The upregulated…”
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A common mechanism allows selective targeting of GluN2B subunit-containing N-methyl-D-aspartate receptors by Schreiber, Julian A., Schepmann, Dirk, Frehland, Bastian, Thum, Simone, Datunashvili, Maia, Budde, Thomas, Hollmann, Michael, Strutz-Seebohm, Nathalie, Wünsch, Bernhard, Seebohm, Guiscard

“…N -methyl- D -aspartate receptors (NMDARs), especially GluN2B-containing NMDARs, are associated with neurodegenerative diseases like Parkinson, Alzheimer and…”
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Computer-assisted design, synthesis, binding and cytotoxicity assessments of new 1-(4-(aryl(methyl)amino)butyl)-heterocyclic sigma 1 ligands by Zampieri, Daniele, Vio, Luciano, Fermeglia, Maurizio, Pricl, Sabrina, Wünsch, Bernhard, Schepmann, Dirk, Romano, Maurizio, Mamolo, Maria Grazia, Laurini, Erik

“…In this work we applied a blend of computational and synthetic techniques with the aim to design, synthesize, and characterize new σ1 receptor (σ1R) ligands…”
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Development of a selective competitive receptor binding assay for the determination of the affinity to NR2B containing NMDA receptors by Schepmann, Dirk, Frehland, Bastian, Lehmkuhl, Kirstin, Tewes, Bastian, Wünsch, Bernhard

“…A selective, rapid and efficient competitive binding assay for the determination of the affinity of compounds towards the ifenprodil binding site of NR2B…”
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Asymmetric Synthesis of 1-Substituted Tetrahydro-3-benzazepines as NMDA Receptor Antagonists by Wirt, Ursula, Schepmann, Dirk, Wünsch, Bernhard

“…A novel asymmetric synthesis of 1‐substituted tetrahydro‐3‐benzazepines (R)‐15 and (S)‐15 has been performed. Starting with o‐phenylenediacetic acid (1) and…”
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Conformationally constrained NR2B selective NMDA receptor antagonists derived from ifenprodil: Synthesis and biological evaluation of tetrahydro-3-benzazepine-1,7-diols by Tewes, Bastian, Frehland, Bastian, Schepmann, Dirk, Schmidtke, Kai-Uwe, Winckler, Thomas, Wünsch, Bernhard

“…NR2B selective NMDA receptor antagonists with tetrahydro-3-benzazepine-1,7-diol scaffold have been designed by formal cleavage and reconstitution of the…”
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Discovery of RC-752, a Novel Sigma-1 Receptor Antagonist with Antinociceptive Activity: A Promising Tool for Fighting Neuropathic Pain by Rossino, Giacomo, Marra, Annamaria, Listro, Roberta, Peviani, Marco, Poggio, Elena, Curti, Daniela, Pellavio, Giorgia, Laforenza, Umberto, Dondio, Giulio, Schepmann, Dirk, Wünsch, Bernhard, Bedeschi, Martina, Marino, Noemi, Tesei, Anna, Ha, Hee-Jin, Kim, Young-Ho, Ann, Jihyae, Lee, Jeewoo, Linciano, Pasquale, Di Giacomo, Marcello, Rossi, Daniela, Collina, Simona

“…Neuropathic pain (NP) is a chronic condition resulting from damaged pain-signaling pathways. It is a debilitating disorder that affects up to 10% of the…”
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Thiazole‐Based σ1 Receptor Ligands: Diversity by Late‐Stage C−H Arylation of Thiazoles, Structure–Affinity and Selectivity Relationships, and Molecular Interactions by Kokornaczyk, Artur K., Schepmann, Dirk, Yamaguchi, Junichiro, Itami, Kenichiro, Laurini, Erik, Fermeglia, Maurizio, Pricl, Sabrina, Wünsch, Bernhard

“…Spirocyclic thiophene derivatives represent promising σ1 ligands with high σ1 affinity and selectivity over the σ2 subtype. To increase ligand efficiency, the…”
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The Action of Reproductive Fluids and Contained Steroids, Prostaglandins, and Zn2+ on CatSper Ca2+ Channels in Human Sperm by Jeschke, Janice K., Biagioni, Cristina, Schierling, Tobias, Wagner, Isabel Viola, Börgel, Frederik, Schepmann, Dirk, Schüring, Andreas, Kulle, Alexandra E., Holterhus, Paul Martin, von Wolff, Michael, Wünsch, Bernhard, Nordhoff, Verena, Strünker, Timo, Brenker, Christoph

“…The sperm-specific Ca 2+ channel CatSper registers chemical cues that assist human sperm to fertilize the egg. Prime examples are progesterone and…”
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Identification, pharmacological evaluation and binding mode analysis of novel chromene and chromane based σ1 receptor ligands by Laurini, Erik, Harel, Dipak, Marson, Domenico, Schepmann, Dirk, Schmidt, Thomas J., Pricl, Sabrina, Wünsch, Bernhard

“…A set of aminoethyl substituted chromenes 3 and chromanes 4, originally developed as antiprotozoal drugs was evaluated as novel types of σ1 receptor ligands…”
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Do GluN2B subunit containing NMDA receptors tolerate a fluorine atom in the phenylalkyl side chain? by Shuto, Yoshihiro, Thum, Simone, Temme, Louisa, Schepmann, Dirk, Kitamura, Masato, Wünsch, Bernhard

“…The influence of an F-atom in the side chain of benzo[7]annulen-7-amines on the affinity towards GluN2B subunit containing NMDA receptors and the selectivity…”
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Chemical, Pharmacological, and in vitro Metabolic Stability Studies on Enantiomerically Pure RC-33 Compounds: Promising Neuroprotective Agents Acting as σ1 Receptor Agonists by Rossi, Daniela, Pedrali, Alice, Gaggeri, Raffaella, Marra, Annamaria, Pignataro, Luca, Laurini, Erik, Dal Col, Valentina, Fermeglia, Maurizio, Pricl, Sabrina, Schepmann, Dirk, Wünsch, Bernhard, Peviani, Marco, Curti, Daniela, Collina, Simona

“…Our recent research efforts identified racemic RC‐33 as a potent and metabolically stable σ1 receptor agonist. Herein we describe the isolation of pure RC‐33…”
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