Search Results - "Schoepp, Darryle"
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mGlu2/3 receptor agonist (LY354740) in anxiety
Published in Pharmacology, biochemistry and behavior (01-09-2024)“…mGlu2/3 Receptors (LY354740) in Anxiety mGlu2/3 receptors when activated decrease glutamate excitation on limbic synapses involved in anxiety. The orally…”
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Activation of mGlu2/3 receptors as a new approach to treat schizophrenia: a randomized Phase 2 clinical trial
Published in Nature medicine (01-09-2007)“…Schizophrenia is a chronic, complex and heterogeneous mental disorder, with pathological features of disrupted neuronal excitability and plasticity within…”
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CNS distribution of metabotropic glutamate 2 and 3 receptors: Transgenic mice and [3H]LY459477 autoradiography
Published in Neuropharmacology (01-03-2013)“…Group II metabotropic glutamate (mGlu) receptor agonists were efficacious in randomized clinical research trials for schizophrenia and generalized anxiety…”
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Evidence for the role of metabotropic glutamate (mGlu)2 not mGlu3 receptors in the preclinical antipsychotic pharmacology of the mGlu2/3 receptor agonist (-)-(1R,4S,5S,6S)-4-amino-2-sulfonylbicyclo[3.1.0]hexane-4,6-dicarboxylic acid (LY404039)
Published in The Journal of pharmacology and experimental therapeutics (01-07-2008)“…(-)-(1R,4S,5S,6S)-4-amino-2-sulfonylbicyclo[3.1.0]hexane-4,6-dicarboxylic acid (LY404039) is a potent and selective group II metabotropic glutamate [(mGlu)2…”
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Efficacy and Tolerability of an mGlu2 3 Agonist in the Treatment of Generalized Anxiety Disorder
Published in Neuropsychopharmacology (New York, N.Y.) (01-06-2008)“…LY354740, a potent and selective mGlu (metabotropic glutamate receptor)2/3 agonist, has shown efficacy in the treatment of generalized anxiety disorder (GAD)…”
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Where will new neuroscience therapies come from?
Published in Nature reviews. Drug discovery (01-10-2011)“…The challenges of developing drugs for central nervous system disorders have led some major companies to reduce or discontinue investment in the field, even…”
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Metabotropic glutamate receptors in the control of mood disorders
Published in CNS & neurological disorders drug targets (01-04-2007)“…Current treatments for depression are less than optimal in terms of onset of action, response and remission rates, and side-effect profiles. Glutamate is the…”
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Metabotropic glutamate receptors as novel targets for anxiety and stress disorders
Published in Nature reviews. Drug discovery (01-02-2005)“…Anxiety and stress disorders are the most commonly occurring of all mental illnesses, and current treatments are less than satisfactory. So, the discovery of…”
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Synaptic Activity Regulates Interstitial Fluid Amyloid-β Levels In Vivo
Published in Neuron (Cambridge, Mass.) (22-12-2005)“…Aggregation of the amyloid-β (Aβ) peptide in the extracellular space of the brain is central to Alzheimer's disease pathogenesis. Aβ aggregation is…”
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Translating glutamate: from pathophysiology to treatment
Published in Science translational medicine (28-09-2011)“…The neurotransmitter glutamate is the primary excitatory neurotransmitter in mammalian brain and is responsible for most corticocortical and corticofugal…”
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Metabotropic glutamate receptors, 5 years on
Published in Neuropharmacology (15-03-2017)Get full text
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In vivo pharmacological characterization of the structurally novel, potent, selective mGlu2/3 receptor agonist LY404039 in animal models of psychiatric disorders
Published in Psychopharmacologia (01-07-2007)“…Data from both preclinical and clinical studies have provided proof of concept that modulation of limbic and forebrain glutamate, via mGlu2/3 receptor…”
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Alzheimer's disease research and development: a call for a new research roadmap
Published in Annals of the New York Academy of Sciences (01-04-2014)“…Epidemiological projections of the prevalence of Alzheimer's disease (AD) and related dementias, the rapidly expanding population over the age of 65, and the…”
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Unveiling the functions of presynaptic metabotropic glutamate receptors in the central nervous system
Published in The Journal of pharmacology and experimental therapeutics (01-10-2001)“…Metabotropic glutamate (mGlu) receptors, which include mGlu1-8 receptors, are a heterogeneous family of G-protein-coupled receptors which function to modulate…”
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Metabotropic glutamate 2 receptor potentiators: receptor modulation, frequency-dependent synaptic activity, and efficacy in preclinical anxiety and psychosis model(s)
Published in Psychopharmacology (01-04-2005)“…To increase subtype selectivity and provide a novel means to alter receptor function, we discovered and characterization potentiators for the metabotropic…”
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Discovery of Allosteric Potentiators for the Metabotropic Glutamate 2 Receptor: Synthesis and Subtype Selectivity of N-(4-(2-Methoxyphenoxy)phenyl)-N-(2,2,2− trifluoroethylsulfonyl)pyrid-3-ylmethylamine
Published in Journal of medicinal chemistry (17-07-2003)“…This report describes recently discovered novel allosteric modulators of metabotropic glutamate2 (mGlu2) receptors. These pyridylmethylsulfonamides (e.g., 3)…”
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Pharmacological and pharmacokinetic properties of a structurally novel, potent, and selective metabotropic glutamate 2/3 receptor agonist: in vitro characterization of agonist (-)-(1R,4S,5S,6S)-4-amino-2-sulfonylbicyclo[3.1.0]-hexane-4,6-dicarboxylic acid (LY404039)
Published in The Journal of pharmacology and experimental therapeutics (01-04-2007)“…Group II metabotropic glutamate (mGlu) receptor agonists, including (1S,2S,5R,6S)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylate monohydrate (LY354740) and…”
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Preclinical pharmacology of mGlu2/3 receptor agonists: novel agents for schizophrenia?
Published in Current drug targets. CNS & neurological disorders (01-04-2002)“…Agonists for mGlu2/3 receptors decrease the evoked release of glutamate at certain (ie. forebrain / limbic) glutamatergic synapses, indicating that the…”
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Effects of mGlu2 or mGlu3 receptor deletions on mGlu2/3 receptor agonist (LY354740)-induced brain c-Fos expression: Specific roles for mGlu2 in the amygdala and subcortical nuclei, and mGlu3 in the hippocampus
Published in Neuropharmacology (01-08-2006)“…LY354740 is a potent and selective mGlu2/3 receptor agonist with activity in models of psychiatric disorders (anxiety, psychosis), and early clinical studies…”
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Regulation of Neurotransmitter Release by Metabotropic Glutamate Receptors
Published in Journal of neurochemistry (01-09-2000)“…: The G protein‐coupled metabotropic glutamate (mGlu) receptors are differentially localized at various synapses throughout the brain. Depending on the…”
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