Search Results - "Alberati, Daniela"
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Glycine Transporter Type I (GlyT1) Inhibitor, Bitopertin: A Journey from Lab to Patient
Published in Chimia (22-08-2018)“…Glycine transporter-1 (GlyT1) inhibition has been extensively studied both in pharmaceutical companies and academic institutions primarily as a potential new…”
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Glycine reuptake inhibitor RG1678: A pharmacologic characterization of an investigational agent for the treatment of schizophrenia
Published in Neuropharmacology (01-02-2012)“…Dysfunctional N-methyl- d-aspartate (NMDA) receptor neurotransmission has been implicated in the pathophysiology of schizophrenia. It is thought that this…”
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Selective GlyT1 Inhibitors: Discovery of [4-(3-Fluoro-5-trifluoromethylpyridin-2-yl)piperazin-1-yl][5-methanesulfonyl-2-((S)-2,2,2-trifluoro-1-methylethoxy)phenyl]methanone (RG1678), a Promising Novel Medicine To Treat Schizophrenia
Published in Journal of medicinal chemistry (24-06-2010)“…The GlyT1 transporter has emerged as a key novel target for the treatment of schizophrenia. Herein, we report on the optimization of the…”
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Prepulse inhibition deficits of the startle reflex in neonatal ventral hippocampal–lesioned rats: reversal by glycine and a glycine transporter inhibitor
Published in Biological psychiatry (1969) (01-12-2003)“…Neonatal ventral hippocampal (NVH) lesions in rats induce behavioral abnormalities at adulthood thought to simulate some aspects of the positive, negative, and…”
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Enhancement of the NMDA receptor function by reduction of glycine transporter-1 expression
Published in Neuroscience letters (03-01-2005)“…The occupation of the glycine binding-site is a prerequisite for NMDA receptor activation by glutamate. To analyze the regulation of NMDA receptor function by…”
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5:45 PM THE NEUROBIOLOGY OF NEGATIVE SYMPTOMS AND THE EFFECT OF GLYCINE REUPTAKE INHIBITORS
Published in Schizophrenia research (01-04-2014)Get full text
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A TRANSLATIONAL SUCCESS STORY: FACILITATING NMDA RECEPTOR SIGNALING WITH THE GLYCINE REUPTAKE INHIBITOR RG1678
Published in Schizophrenia research (01-04-2012)Get full text
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Effect of bitopertin, a glycine reuptake inhibitor, on negative symptoms of schizophrenia: a randomized, double-blind, proof-of-concept study
Published in JAMA psychiatry (Chicago, Ill.) (01-06-2014)“…In schizophrenia, the severity of negative symptoms is a key predictor of long-term disability. Deficient signaling through the N-methyl-D-aspartate receptor…”
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Assessment of a glycine uptake inhibitor in animal models of effort-related choice behavior: implications for motivational dysfunctions
Published in Psychopharmacology (01-05-2017)“…Rationale Motivated behavior can be characterized by a substantial exertion of effort, and organisms often make effort-related decisions based upon analyses of…”
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Effects of the glycine reuptake inhibitors bitopertin and RG7118 on glycine in cerebrospinal fluid: results of two proofs of mechanism studies in healthy volunteers
Published in Psychopharmacology (01-07-2016)“…Rationale Hypofunction of NMDA receptors has been implicated in neuropsychiatric disorders including schizophrenia. NMDA receptor neurotransmission can be…”
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Effects of GlyT1 inhibition on erythropoiesis and iron homeostasis in rats
Published in Experimental hematology (01-10-2016)“…Glycine is a key rate-limiting component of heme biosynthesis in erythropoietic cells, where the high intracellular glycine demand is primarily supplied by the…”
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Preclinical Reproductive and Developmental Toxicity Profile of a Glycine Transporter Type 1 (Glyt1) Inhibitor
Published in Birth defects research. Part B. Developmental and reproductive toxicology (01-06-2016)“…Bitopertin is a glycine type 1 (GlyT1) inhibitor intended for the treatment of psychiatric disorders. The principle adverse effect in the regulatory…”
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Physiologically Based Pharmacokinetic Modelling to Predict Single- and Multiple-Dose Human Pharmacokinetics of Bitopertin
Published in Clinical pharmacokinetics (01-08-2013)“…Background Bitopertin (RG1678) is a glycine reuptake inhibitor currently in phase 3 trials for treatment of schizophrenia. This paper describes the use of…”
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Alterations in High-Frequency Neuronal Oscillations in a Cynomolgus Macaque Test of Sustained Attention Following NMDA Receptor Antagonism
Published in Neuropsychopharmacology (New York, N.Y.) (01-04-2016)“…A growing body of evidence indicates that neuronal oscillations in the gamma frequency range (30-80 Hz) are disturbed in schizophrenic patients during…”
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Pre-clinical characterization of [11C]R05013853 as a novel radiotracer for imaging of the glycine transporter type 1 by positron emission tomography
Published in NeuroImage (Orlando, Fla.) (15-07-2013)“…A specific positron emission tomography (PET) radiotracer for the glycine transporter type 1 (GlyT1) would constitute an imaging biomarker to investigate the…”
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Pharmacological evaluation of a novel assay for detecting glycine transporter 1 inhibitors and their antipsychotic potential
Published in Pharmacology, biochemistry and behavior (01-12-2010)“…Multiple lines of evidence support the notion that hypofunction of glutamatergic neurotransmission is involved in the pathophysiology of schizophrenia…”
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Regulation of the kynurenine metabolic pathway by interferon-gamma in murine cloned macrophages and microglial cells
Published in Journal of neurochemistry (01-03-1996)“…Several pieces of evidence suggest a major role for brain macrophages in the overproduction of neuroactive kynurenines, including quinolinic acid, in brain…”
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[11C]-RO5013853: a New PET Radioligand for the Glycine Transporter TYPE 1
Published in Neuropsychopharmacology (New York, N.Y.) (01-08-2014)Get full text
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Erratum: [11C]-RO5013853: a New PET Radioligand for the Glycine Transporter TYPE 1
Published in Neuropsychopharmacology (New York, N.Y.) (16-07-2014)Get full text
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