Basmisanil, a highly selective GABAA-α5 negative allosteric modulator: preclinical pharmacology and demonstration of functional target engagement in man

Autor: Joerg F. Hipp, Frederic Knoflach, Robert Comley, Theresa M. Ballard, Michael Honer, Gerhard Trube, Rodolfo Gasser, Eric Prinssen, Tanya L. Wallace, Andreas Rothfuss, Henner Knust, Sian Lennon-Chrimes, Michael Derks, Darren Bentley, Lisa Squassante, Stephane Nave, Jana Nöldeke, Christoph Wandel, Andrew W. Thomas, Maria-Clemencia Hernandez

Publikováno v: Scientific Reports, Vol 11, Iss 1, Pp 1-20 (2021)

Abstract GABAA-α5 subunit-containing receptors have been shown to play a key modulatory role in cognition and represent a promising drug target for cognitive dysfunction, as well as other disorders. Here we report on the preclinical and early clinic

Externí odkaz: https://doaj.org/article/1cc826ca236941e185deaad9d64c993b

Preclinical and Clinical Pharmacology of Basmisanil, a Novel Selective GABAA-α5 Receptor Negative Allosteric Modulator

Autor: Christoph Wandel, Michael Honer, Michael Derks, Frédéric Knoflach, Rodolfo Gasser, Gerhard Trube, Stephane Nave, Eric Prinssen, Joerg F. Hipp, Jana Noeldeke, Lisa Squassante, Henner Knust, Andrew Thomas, Tanya L. Wallace, Theresa M. Ballard, Maria-Clemencia Hernandez, Andreas Rothfuss, Robert A. Comley, Sian Lennon-Chrimes

Background and Purpose GABAA-α5 subunit-containing receptors have been shown to play a key modulatory role in cognition and represent a promising drug target for cognitive dysfunction, as well as other disorders. We describe the preclinical and clin

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::77f3de28ddfb81f3c6a817b4bbcffe23
https://doi.org/10.22541/au.159492919.93709869

Evolution of a maternal immune activation (mIA) model in rats:early developmental effects

Autor: Varsha Mason, Patrick C McHugh, Maurizio Manca, Katie N. Murray, Michael K. Harte, Ben Grayson, Michelle E. Edye, Joanna C. Neill, Eric Prinssen, Reinmar Hager, Anthony C. Vernon, Victoria Fasolino, Joanna M. Oladipo, Irene Knuesel

Publikováno v: Murray, K N, Edye, M E, Manca, M, Vernon, A C, Oladipo, J M, Fasolino, V, Harte, M K, Mason, V, Grayson, B, McHugh, P C, Knuesel, I, Prinssen, E P, Hager, R & Neill, J C 2019, ' Evolution of a maternal immune activation (mIA) model in rats : early developmental effects ', Brain, Behavior, and Immunity, vol. 75, no. 0, pp. 48-59 . https://doi.org/10.1016/j.bbi.2018.09.005
Murray, K N, Edye, M E, Manca, M, Vernon, A C, Oladipo, J M, Fasolino, V, Harte, M K, Mason, V, Grayson, B, Mchugh, P C, Knuesel, I, Prinssen, E P, Hager, R & Neill, J C 2019, ' Evolution of a maternal immune activation (mIA) model in rats: Early developmental effects ', Brain, Behavior, and Immunity, vol. 75, pp. 48-59 . https://doi.org/10.1016/j.bbi.2018.09.005

Maternal immune activation (mIA) in rodents is rapidly emerging as a key model for neurodevelopmental disorders such as autism spectrum disorder (ASD) and schizophrenia. Here, we optimise a mIA model in rats, aiming to address certain limitations of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fdfd0788d57515ad8ac5dfeab3c54494
https://kclpure.kcl.ac.uk/ws/files/101174717/Evolution_of_a_maternal_immune_MURRAY_Firstonline12September2018_GREEN_AAM_CC_BY_NC_ND_.pdf

Metabotropic Glutamate Receptor 5 Negative Allosteric Modulators: Discovery of 2-Chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (Basimglurant, RO4917523), a Promising Novel Medicine for Psychiatric Diseases

Autor: Georg Jaeschke, Urs Niederhauser, Beatrice David, Eric Vieira, Will Spooren, Martin Kuratli, Jens-Uwe Peters, Michael Honer, Wolfgang Guba, Thomas Hartung, Daniel Tännler, Christoph Funk, Nadia Bitter-Stoll, Porter Richard Hugh Phillip, Bernd Büttelmann, Daniel Rueher, Paul Spurr, Jörg Huwyler, Nicole Clemann, Eric Prinssen, Joseph G. Wettstein, Axel Pähler, Simona M. Ceccarelli, Patrick Boissin, Theodor Stoll, Antonio Ricci, Jürgen Wichmann, Ann Petersen, Manfred Schneider, Marianne Rueher, Edilio Borroni, Sabine Kolczewski, Anthony Harrison, Lothar Lindemann

Publikováno v: Journal of Medicinal Chemistry. 58:1358-1371

Negative allosteric modulators (NAMs) of metabotropic glutamate receptor 5 (mGlu5) have potential for the treatment of psychiatric diseases including depression, fragile X syndrome (FXS), anxiety, obsessive-compulsive disorders, and levodopa induced

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f629d43eba9d48337f793d5244811596
https://doi.org/10.1021/jm501642c

Sembragiline: A Novel, Selective Monoamine Oxidase Type B Inhibitor for the Treatment of Alzheimer's Disease

Autor: Bart A. Ellenbroek, Axel Pähler, Bernd Bohrmann, Hansruedi Loetscher, Edilio Borroni, Wyler Rene, Julie K. Andersen, Juerg Messer, Anand Rane, Andrea M. Cesura, Stephane Nave, Fiona Grueninger, Subramanian Rajagopalan, Shankar J. Chinta, Eric Prinssen, Almas Siddiqui

Publikováno v: The Journal of pharmacology and experimental therapeutics. 362(3)

Monoamine oxidase B (MAO-B) has been implicated in the pathogenesis of Alzheimer's disease (AD) and other neurodegenerative disorders. Increased MAO-B expression in astroglia has been observed adjacent to amyloid plaques in AD patient brains. This ph

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8aacf63885b6c44711a1262e8f93416f
https://pubmed.ncbi.nlm.nih.gov/28642233