Search Results - "Auberson, Yves P."
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Improving Nonspecific Binding and Solubility: Bicycloalkyl Groups and Cubanes as para‐Phenyl Bioisosteres
Published in ChemMedChem (20-04-2017)“…Bicycloalkyl groups have been previously described as phenyl group bioisosteres. This article describes the synthesis of new building blocks allowing their…”
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The role of GluN2A and GluN2B subunits on the effects of NMDA receptor antagonists in modeling schizophrenia and treating refractory depression
Published in Neuropsychopharmacology (New York, N.Y.) (01-10-2014)“…Paradoxically, N-methyl-D-aspartate (NMDA) receptor antagonists are used to model certain aspects of schizophrenia as well as to treat refractory depression…”
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Reduced Metabotropic Glutamate Receptor 5 Density in Major Depression Determined by [11C]ABP688 PET and Postmortem Study
Published in The American journal of psychiatry (01-07-2011)“…Clinical and preclinical evidence suggests a hyperactive glutamatergic system in clinical depression. Recently, the metabotropic glutamate receptor 5 (mGluR5)…”
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Regional brain mGlu5 receptor occupancy following single oral doses of mavoglurant as measured by [11C]-ABP688 PET imaging in healthy volunteers
Published in NeuroImage (Orlando, Fla.) (15-04-2021)“…•Mavoglurant binds to same allosteric site on mGluR5 as the radioligand [11C]-ABP688.•Mavoglurant penetrates brain and induces mGluR5 receptors occupancy in…”
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Role of NMDA Receptor Subtypes in Governing the Direction of Hippocampal Synaptic Plasticity
Published in Science (American Association for the Advancement of Science) (14-05-2004)“…Activation of N-methyl-D-aspartate subtype glutamate receptors (NMDARs) is required for long-term potentiation (LTP) and long-term depression (LTD) of…”
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Enhanced Astrocytic Ca2+ Signals Contribute to Neuronal Excitotoxicity after Status Epilepticus
Published in The Journal of neuroscience (03-10-2007)“…Status epilepticus (SE), an unremitting seizure, is known to cause a variety of traumatic responses including delayed neuronal death and later cognitive…”
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Medicinal Chemists Don't Just Make Drugs - The Art of Developing Low Molecular Weight Imaging Agents in Switzerland
Published in Chimia (21-12-2016)“…Radiolabeled molecular imaging agents are useful to study drug distribution, target engagement and disease progression in human patients. Medicinal chemists…”
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Zinc Modulates Bidirectional Hippocampal Plasticity by Effects on NMDA Receptors
Published in The Journal of neuroscience (05-07-2006)“…Zinc has complex effects on NMDA receptors (NMDARs) and may be an endogenous modulator of synaptic plasticity. In the CA1 region of rat hippocampal slices, we…”
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mGluR5 stimulates gliotransmission in the nucleus accumbens
Published in Proceedings of the National Academy of Sciences - PNAS (06-02-2007)“…Although metabotropic glutamate receptor 5 (mGluR5) is essential for cocaine self-administration and drug-seeking behavior, there is limited knowledge of the…”
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Signaling pathways responsible for the rapid antidepressant-like effects of a GluN2A-preferring NMDA receptor antagonist
Published in Translational psychiatry (18-04-2018)“…In a previous study we found that the preferring GluN2A receptor antagonist, NVP-AAM077, elicited rapid antidepressant-like effects in the forced swim test…”
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Differential Roles of NR2A and NR2B-Containing NMDA Receptors in Cortical Long-Term Potentiation and Long-Term Depression
Published in The Journal of neuroscience (08-09-2004)“…It is widely believed that long-term depression (LTD) and its counterpart, long-term potentiation (LTP), involve mechanisms that are crucial for learning and…”
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Fostering Research Synergies between Chemists in Swiss Academia and at Novartis
Published in Chimia (01-11-2021)“…We present a short overview of the way Novartis chemists interact and collaborate with the academic chemistry community in Switzerland. This article…”
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Preclinical Evaluation of Benzazepine-Based PET Radioligands (R)- and (S)-11C-Me-NB1 Reveals Distinct Enantiomeric Binding Patterns and a Tightrope Walk Between GluN2B- and σ1-Receptor–Targeted PET Imaging
Published in The Journal of nuclear medicine (1978) (01-08-2019)“…The study aims to investigate the performance characteristics of the enantiomers of 11C-Me-NB1, a recently reported PET imaging probe that targets the GluN2B…”
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Double Dissociation of Spike Timing–Dependent Potentiation and Depression by Subunit-Preferring NMDA Receptor Antagonists in Mouse Barrel Cortex
Published in Cerebral cortex (New York, N.Y. 1991) (01-12-2009)“…Spike timing–dependent plasticity (STDP) is a strong candidate for an N-methyl-D-aspartate (NMDA) receptor-dependent form of synaptic plasticity that could…”
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Upregulation of Forebrain NMDA NR2B Receptors Contributes to Behavioral Sensitization after Inflammation
Published in The Journal of neuroscience (30-11-2005)“…Transgenic overexpression of NMDA NR2B receptors in forebrain regions increased behavioral responses to persistent inflammatory pain. However, it is not known…”
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MS565: A SPECT Tracer for Evaluating the Brain Penetration of BAF312 (Siponimod)
Published in ChemMedChem (01-06-2015)“…BAF312 (siponimod) is a sphingosine‐1‐phosphate (S1P) receptor modulator in clinical development for the treatment of multiple sclerosis, with faster…”
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Blockade of NMDA Receptors 2A Subunit in the Dorsal Striatum Impairs the Learning of a Complex Motor Skill
Published in Behavioral neuroscience (01-10-2011)“…Accumulating evidence proposes that the striatum, known to control voluntary movement, may also play a role in learning and memory. Striatum learning is…”
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EFMC, Medicinal Chemistry and Chemical Biology in Europe
Published in ChemMedChem (15-12-2020)“…This article is a reflection on the development of medicinal chemistry and chemical biology in Europe, and how the European Federation for Medicinal Chemistry…”
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ABP688, a novel selective and high affinity ligand for the labeling of mGlu5 receptors: Identification, in vitro pharmacology, pharmacokinetic and biodistribution studies
Published in Bioorganic & medicinal chemistry (15-01-2007)“…[ 11C]ABP688 ( 2) has recently been demonstrated to be a useful PET tracer for in vivo imaging of the metabotropic glutamate receptors type 5 (mGluR5) in…”
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The Different Effects on Recognition Memory of Perirhinal Kainate and NMDA Glutamate Receptor Antagonism: Implications for Underlying Plasticity Mechanisms
Published in The Journal of neuroscience (29-03-2006)“…To investigate the involvement of different types of glutamate receptors in recognition memory, selective antagonists of NMDA and kainate receptors were…”
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