Search Results - "Ofner, Silvio"

Blocking Metabotropic Glutamate Receptor Subtype 7 (mGlu7) via the Venus Flytrap Domain (VFTD) Inhibits Amygdala Plasticity, Stress, and Anxiety-related Behavior by Gee, Christine E., Peterlik, Daniel, Neuhäuser, Christoph, Bouhelal, Rochdi, Kaupmann, Klemens, Laue, Grit, Uschold-Schmidt, Nicole, Feuerbach, Dominik, Zimmermann, Kaspar, Ofner, Silvio, Cryan, John F., van der Putten, Herman, Fendt, Markus, Vranesic, Ivo, Glatthar, Ralf, Flor, Peter J.

“…The metabotropic glutamate receptor subtype 7 (mGlu7) is an important presynaptic regulator of neurotransmission in the mammalian CNS. mGlu7 function has been…”
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A Selective Metabotropic Glutamate Receptor 7 Agonist: Activation of Receptor Signaling via an Allosteric Site Modulates Stress Parameters In vivo by Kayo Mitsukawa, Rina Yamamoto, Silvio Ofner, Joachim Nozulak, Oliver Pescott, Snezana Lukic, Natacha Stoehr, Cedric Mombereau, Kuhn, Rainer, Kevin H. Mc Allister, van der Putten, Herman, Cryan, John F., Peter J. Flor, Scolnick, Edward M.

“…Metabotropic glutamate receptor (mGluR) subtypes (mGluRI to mGluR8) act as important pre- and postsynaptic regulators of neurotransmission in the CNS. These…”
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Distinct effects of IPSU and suvorexant on mouse sleep architecture by Hoyer, Daniel, Dürst, Thomas, Fendt, Markus, Jacobson, Laura H, Betschart, Claudia, Hintermann, Samuel, Behnke, Dirk, Cotesta, Simona, Laue, Grit, Ofner, Silvio, Legangneux, Eric, Gee, Christine E

“…Dual orexin receptor (OXR) antagonists (DORAs) such as almorexant, SB-649868, suvorexant (MK-4305), and filorexant (MK-6096), have shown promise for the…”
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Kinetic properties of "dual" orexin receptor antagonists at OX1R and OX2R orexin receptors by Callander, Gabrielle E, Olorunda, Morenike, Monna, Dominique, Schuepbach, Edi, Langenegger, Daniel, Betschart, Claudia, Hintermann, Samuel, Behnke, Dirk, Cotesta, Simona, Fendt, Markus, Laue, Grit, Ofner, Silvio, Briard, Emmanuelle, Gee, Christine E, Jacobson, Laura H, Hoyer, Daniel

“…Orexin receptor antagonists represent attractive targets for the development of drugs for the treatment of insomnia. Both efficacy and safety are crucial in…”
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Pharmacological Characterization of Some Selected 4,5-Dihydro-4-oxo-1,2,4-triazolo[1,5-a]quinoxaline-2-carboxylates and 3-Hydroxyquinazoline-2,4-diones as (S)-2-Amino-3-(3-hydroxy-5-methylisoxazol-4-yl)-propionic Acid Receptor Antagonists by Catarzi, Daniela, Lenzi, Ombretta, Colotta, Vittoria, Varano, Flavia, Poli, Daniela, Filacchioni, Guido, Lingenhöhl, Kurt, Ofner, Silvio

“…In the present study, some selected, previously reported 4,5-dihydro-4-oxo-1,2,4-triazolo[1,5-a]quinoxaline-2-carboxylates (TQXs) and…”
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AFQ056/mavoglurant, a novel clinically effective mGluR5 antagonist: Identification, SAR and pharmacological characterization by Vranesic, Ivo, Ofner, Silvio, Flor, Peter Josef, Bilbe, Graeme, Bouhelal, Rochdi, Enz, Albert, Desrayaud, Sandrine, McAllister, Kevin, Kuhn, Rainer, Gasparini, Fabrizio

“…[Display omitted] Here we describe the identification, structure–activity relationship and the initial pharmacological characterization of AFQ056/mavoglurant,…”
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Identification of a Novel Series of Orexin Receptor Antagonists with a Distinct Effect on Sleep Architecture for the Treatment of Insomnia by Betschart, Claudia, Hintermann, Samuel, Behnke, Dirk, Cotesta, Simona, Fendt, Markus, Gee, Christine E, Jacobson, Laura H, Laue, Grit, Ofner, Silvio, Chaudhari, Vinod, Badiger, Sangamesh, Pandit, Chetan, Wagner, Juergen, Hoyer, Daniel

“…Dual orexin receptor (OXR) antagonists (DORAs) such as almorexant, 1 (SB-649868), or suvorexant have shown promise for the treatment of insomnias and sleep…”
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The Crystal Structure of Cancer Osaka Thyroid Kinase Reveals an Unexpected Kinase Domain Fold by Gutmann, Sascha, Hinniger, Alexandra, Fendrich, Gabriele, Drückes, Peter, Antz, Sylvie, Mattes, Henri, Möbitz, Henrik, Ofner, Silvio, Schmiedeberg, Niko, Stojanovic, Aleksandar, Rieffel, Sebastien, Strauss, André, Troxler, Thomas, Glatthar, Ralf, Sparrer, Helmut

“…Macrophages are important cellular effectors in innate immune responses and play a major role in autoimmune diseases such as rheumatoid arthritis. Cancer Osaka…”
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A General Strategy for Targeting Drugs to Bone by Jahnke, Wolfgang, Bold, Guido, Marzinzik, Andreas L., Ofner, Silvio, Pellé, Xavier, Cotesta, Simona, Bourgier, Emmanuelle, Lehmann, Sylvie, Henry, Chrystelle, Hemmig, René, Stauffer, Frédéric, Hartwieg, J. Constanze D., Green, Jonathan R., Rondeau, Jean-Michel

“…Targeting drugs to their desired site of action can increase their safety and efficacy. Bisphosphonates are prototypical examples of drugs targeted to bone…”
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Quinazolinedione sulfonamides: A novel class of competitive AMPA receptor antagonists with oral activity by Koller, Manuel, Lingenhoehl, Kurt, Schmutz, Markus, Vranesic, Ivan-Toma, Kallen, Joerg, Auberson, Yves P., Carcache, David A., Mattes, Henri, Ofner, Silvio, Orain, David, Urwyler, Stephan

“…Quinazoline-2,4-diones with a sulfonamide group attached to the N(3) ring atom constitute a novel class of competitive AMPA receptor antagonists. One of the…”
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Discovery of Novel Allosteric Non-Bisphosphonate Inhibitors of Farnesyl Pyrophosphate Synthase by Integrated Lead Finding by Marzinzik, Andreas L., Amstutz, René, Bold, Guido, Bourgier, Emmanuelle, Cotesta, Simona, Glickman, J. Fraser, Götte, Marjo, Henry, Christelle, Lehmann, Sylvie, Hartwieg, J. Constanze D., Ofner, Silvio, Pellé, Xavier, Roddy, Thomas P., Rondeau, Jean-Michel, Stauffer, Frédéric, Stout, Steven J., Widmer, Armin, Zimmermann, Johann, Zoller, Thomas, Jahnke, Wolfgang

“…Farnesyl pyrophosphate synthase (FPPS) is an established target for the treatment of bone diseases, but also shows promise as an anticancer and anti‐infective…”
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6-Amino quinazolinedione sulfonamides as orally active competitive AMPA receptor antagonists by Orain, David, Ofner, Silvio, Koller, Manuel, Carcache, David A., Froestl, Wolfgang, Allgeier, Hans, Rasetti, Vittorio, Nozulak, Joachim, Mattes, Henri, Soldermann, Nicolas, Floersheim, Philipp, Desrayaud, Sandrine, Kallen, Joerg, Lingenhoehl, Kurt, Urwyler, Stephan

“…A new set of quinazolinedione sulfonamide derivatives as competitive AMPA receptor antagonist with improved properties compared to 1 is disclosed. By…”
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Gezielte Anreicherung von Wirkstoffen am Knochen am Beispiel von allosterischen FPPS‐Inhibitoren by Jahnke, Wolfgang, Bold, Guido, Marzinzik, Andreas L., Ofner, Silvio, Pellé, Xavier, Cotesta, Simona, Bourgier, Emmanuelle, Lehmann, Sylvie, Henry, Chrystelle, Hemmig, René, Stauffer, Frédéric, Hartwieg, J. Constanze D., Green, Jonathan R., Rondeau, Jean‐Michel

“…Die Wirksamkeit und Verträglichkeit eines Medikaments kann verbessert werden, indem dieses gezielt an den gewünschten Wirkungsort gebracht wird. Bisphosphonate…”
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NKP608: a selective NK-1 receptor antagonist with anxiolytic-like effects in the social interaction and social exploration test in rats by Vassout, Annick, Veenstra, Siem, Hauser, Kathleen, Ofner, Silvio, Brugger, Felix, Schilling, Walter, Gentsch, Conrad

“…NKP608 is a non-peptidic derivative of 4-aminopiperidine which acts as a selective, specific and potent antagonist at the neurokinin-1 (NK-1) receptor both in…”
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Gezielte Anreicherung von Wirkstoffen am Knochen am Beispiel von allosterischen FPPS-Inhibitoren by Jahnke, Wolfgang, Bold, Guido, Marzinzik, Andreas L., Ofner, Silvio, Pellé, Xavier, Cotesta, Simona, Bourgier, Emmanuelle, Lehmann, Sylvie, Henry, Chrystelle, Hemmig, René, Stauffer, Frédéric, Hartwieg, J. Constanze D., Green, Jonathan R., Rondeau, Jean-Michel

“…Abstract Die Wirksamkeit und Verträglichkeit eines Medikaments kann verbessert werden, indem dieses gezielt an den gewünschten Wirkungsort gebracht wird…”
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N-Phosphonoalkyl-5-aminomethylquinoxaline-2,3-diones: In vivo active AMPA and NMDA(glycine) antagonists by Auberson, Yves P., Acklin, Pierre, Bischoff, Serge, Moretti, Robert, Ofner, Silvio, Schmutz, Markus, Veenstra, Siem J.

“…N-Substituted 5-aminomethylquinoxalinediones containing carboxy or phosphonic acids yield potent and selective AMPA and/or NMDA (glycine-binding site)…”
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SAR of 2-benzyl-4-aminopiperidines: CGP 49823, an orally and centrally active non-peptide NK1 antagonist by Ofner, Silvio, Hauser, Kathleen, Schilling, Walter, Vassout, Annick, Veenstra, Siem J.

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5-aminomethylquinoxaline-2,3-diones, Part III: Arylamide derivatives as highly potent and selective glycine-site NMDA receptor antagonists by Acklin, Pierre, Allgeier, Hans, Auberson, Yves P., Bischoff, Serge, Ofner, Silvio, Sauer, Dirk, Schmutz, Markus

“…A series of quinoxaline-2,3-diones with very high affinity to the glycine site of the NMDA receptor has been discovered. In contrast to the 7-nitro…”
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5-aminomethylquinoxaline-2,3-diones. Part II: N-aryl derivatives as novel NMDA/glycine and AMPA antagonists by Auberson, Yves P, Acklin, Pierre, Allgeier, Hans, Biollaz, Michel, Bischoff, Serge, Ofner, Silvio, Veenstra, Siem J

“…Potent antagonists at the glycine-binding site of NMDA receptors, as well as dual antagonists acting also at AMPA receptors have been identified in a series of…”
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SAR of 2-benzyl-4-aminopiperidines NK1 antagonists. Part 21. synthesis of CGP 49823 by Veenstra, Siem J., Hauser, Kathleen, Schilling, Walter, Betschart, Claudia, Ofner, Silvio

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