The Use of Physiology-Based Pharmacokinetic and Pharmacodynamic Modeling in the Discovery of the Dual Orexin Receptor Antagonist ACT-541468
Treiber, Alexander, de Kanter, Ruben, Roch, Catherine, Gatfield, John, Boss, Christoph, von Raumer, Markus, Schindelholz, Benno, Muehlan, Clemens, van Gerven, Joop, Jenck, Francois
Published in The Journal of pharmacology and experimental therapeutics (01.09.2017)
Published in The Journal of pharmacology and experimental therapeutics (01.09.2017)
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Journal Article
Biomedical Application of Orexin/Hypocretin Receptor Ligands in Neuroscience
Boss, Christoph, Brisbare-Roch, Catherine, Jenck, Francois
Published in Journal of medicinal chemistry (26.02.2009)
Published in Journal of medicinal chemistry (26.02.2009)
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Journal Article
Orexin Receptor Antagonists: A New Concept In CNS Disorders?
Gatfield, John, Brisbare-Roch, Catherine, Jenck, Francois, Boss, Christoph
Published in ChemMedChem (02.08.2010)
Published in ChemMedChem (02.08.2010)
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Journal Article
Structure-Activity Relationship, Biological, and Pharmacological Characterization of the Proline Sulfonamide ACT-462206: a Potent, Brain-Penetrant Dual Orexin 1/Orexin 2 Receptor Antagonist
Boss, Christoph, Roch-Brisbare, Catherine, Steiner, Michel A., Treiber, Alexander, Dietrich, Hendrik, Jenck, Francois, von Raumer, Markus, Sifferlen, Thierry, Brotschi, Christine, Heidmann, Bibia, Williams, Jodi T., Aissaoui, Hamed, Siegrist, Romain, Gatfield, John
Published in ChemMedChem (01.11.2014)
Published in ChemMedChem (01.11.2014)
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Journal Article
Structure–activity relationship studies and sleep-promoting activity of novel 1-chloro-5,6,7,8-tetrahydroimidazo[1,5-a]pyrazine derivatives as dual orexin receptor antagonists. Part 2
Sifferlen, Thierry, Koberstein, Ralf, Cottreel, Emmanuelle, Boller, Amandine, Weller, Thomas, Gatfield, John, Brisbare-Roch, Catherine, Jenck, Francois, Boss, Christoph
Published in Bioorganic & medicinal chemistry letters (01.07.2013)
Published in Bioorganic & medicinal chemistry letters (01.07.2013)
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Journal Article
Synthesis, structure–activity relationship studies, and identification of novel 5,6,7,8-tetrahydroimidazo[1,5-a]pyrazine derivatives as dual orexin receptor antagonists. Part 1
Sifferlen, Thierry, Koberstein, Ralf, Cottreel, Emmanuelle, Boller, Amandine, Weller, Thomas, Gatfield, John, Brisbare-Roch, Catherine, Jenck, Francois, Boss, Christoph
Published in Bioorganic & medicinal chemistry letters (01.04.2013)
Published in Bioorganic & medicinal chemistry letters (01.04.2013)
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Journal Article
Targeted Disruption of the Orphanin FQ/Nociceptin Gene Increases Stress Susceptibility and Impairs Stress Adaptation in Mice
Koster, Anja, Montkowski, Alexandra, Schulz, Stefan, Stube, Eva-Maria, Knaudt, Kristina, Jenck, Francois, Moreau, Jean-Luc, Nothacker, Hans-Peter, Civelli, Olivier, Reinscheid, Rainer K.
Published in Proceedings of the National Academy of Sciences - PNAS (31.08.1999)
Published in Proceedings of the National Academy of Sciences - PNAS (31.08.1999)
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Journal Article
Orphanin FQ Acts as an Anxiolytic to Attenuate Behavioral Responses to Stress
Jenck, F, Moreau, J L, Martin, J R, Kilpatrick, G J, Reinscheid, R K, Monsma, Jr, F J, Nothacker, H P, Civelli, O
Published in Proceedings of the National Academy of Sciences - PNAS (23.12.1997)
Published in Proceedings of the National Academy of Sciences - PNAS (23.12.1997)
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Journal Article
Discovery and Characterization of ACT-335827, an Orally Available, Brain Penetrant Orexin Receptor Type 1 Selective Antagonist
Steiner, Michel A., Gatfield, John, Brisbare-Roch, Catherine, Dietrich, Hendrik, Treiber, Alexander, Jenck, Francois, Boss, Christoph
Published in ChemMedChem (01.06.2013)
Published in ChemMedChem (01.06.2013)
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Journal Article
Promotion of sleep by targeting the orexin system in rats, dogs and humans
Jenck, François, Brisbare-Roch, Catherine, Dingemanse, Jasper, Koberstein, Ralf, Hoever, Petra, Aissaoui, Hamed, Flores, Susan, Mueller, Celia, Nayler, Oliver, van Gerven, Joop, de Haas, Sanne L, Hess, Patrick, Qiu, Changbin, Buchmann, Stephan, Scherz, Michael, Weller, Thomas, Fischli, Walter, Clozel, Martine
Published in Nature medicine (01.02.2007)
Published in Nature medicine (01.02.2007)
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Journal Article
Orexin Receptor Antagonism: A New Principle in Neuroscience
Christoph Boss, Catherine Brisbare-Roch, Francois Jenck, Hamed Aissaoui, Ralf Koberstein, Thierry Sifferlen, Thomas Weller
Published in Chimia (01.01.2008)
Published in Chimia (01.01.2008)
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Journal Article
The dual orexin receptor antagonist almorexant, alone and in combination with morphine, cocaine and amphetamine, on conditioned place preference and locomotor sensitization in the rat
Steiner, Michel Alexander, Lecourt, Hugues, Jenck, François
Published in The international journal of neuropsychopharmacology (01.03.2013)
Published in The international journal of neuropsychopharmacology (01.03.2013)
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Journal Article
Pharmacological Characterization of the Novel Nonpeptide Orphanin FQ/Nociceptin Receptor Agonist Ro 64-6198: Rapid and Reversible Desensitization of the ORL1 Receptor in Vitro and Lack of Tolerance in Vivo
Dautzenberg, F M, Wichmann, J, Higelin, J, Py-Lang, G, Kratzeisen, C, Malherbe, P, Kilpatrick, G J, Jenck, F
Published in The Journal of pharmacology and experimental therapeutics (01.08.2001)
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Published in The Journal of pharmacology and experimental therapeutics (01.08.2001)
Journal Article
Functional Consequences of Reduction in NMDA Receptor Glycine Affinity in Mice Carrying Targeted Point Mutations in the Glycine Binding Site
Kew, James N. C, Koester, Anja, Moreau, Jean-Luc, Jenck, Francois, Ouagazzal, Abdel-Mouttalib, Mutel, Vincent, Richards, J. Grayson, Trube, Gerhard, Fischer, Guenther, Montkowski, Alexandra, Hundt, Wolfgang, Reinscheid, Rainer K, Pauly-Evers, Meike, Kemp, John A, Bluethmann, Horst
Published in The Journal of neuroscience (01.06.2000)
Published in The Journal of neuroscience (01.06.2000)
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Journal Article
002 Daridorexant, a dual orexin receptor antagonist, improves age-related insomnia in rats
Roch, Catherine, Fischer, Cédric, Jenck, Francois, Steiner, Michel
Published in Sleep (New York, N.Y.) (03.05.2021)
Published in Sleep (New York, N.Y.) (03.05.2021)
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Journal Article
Discovery of Highly Potent Dual Orexin Receptor Antagonists via a Scaffold-Hopping Approach
Heidmann, Bibia, Gatfield, John, Roch, Catherine, Treiber, Alexander, Tortoioli, Simone, Brotschi, Christine, Williams, Jodi T., Bolli, Martin H., Abele, Stefan, Sifferlen, Thierry, Jenck, François, Boss, Christoph
Published in ChemMedChem (06.10.2016)
Published in ChemMedChem (06.10.2016)
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Journal Article
A Synthetic Agonist at the Orphanin FQ/Nociceptin Receptor ORL1: Anxiolytic Profile in the Rat
Jenck, Francois, Wichmann, Juergen, Dautzenberg, Frank M., Moreau, Jean-Luc, Ouagazzal, Abdel M., Martin, James R., Lundstrom, Kenneth, Cesura, Andrea M., Poli, Sonia M., Roever, Stephan, Kolczewski, Sabine, Adam, Geo, Kilpatrick, Gavin
Published in Proceedings of the National Academy of Sciences - PNAS (25.04.2000)
Published in Proceedings of the National Academy of Sciences - PNAS (25.04.2000)
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