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Metabotropic glutamate receptor

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https://www.readbyqxmd.com/read/29350927/synthesis-and-pharmacological-characterization-of-c4%C3%AE-amide-substituted-2-aminobicyclo-3-1-0-hexane-2-6-dicarboxylates-identification-of-1s-2s-4s-5r-6s-2-amino-4-3-methoxybenzoyl-amino-bicyclo-3-1-0-hexane-2-6-dicarboxylic-acid-ly2794193-a-highly-potent-and
#1
James A Monn, Steven S Henry, Steven M Massey, David K Clawson, Qi Chen, Benjamin A Diseroad, Rajni M Bhardwaj, Shane Atwell, Frances Lu, Jing Wang, Marijane Russell, Beverly A Heinz, Xu-Shan Wang, Joan H Carter, Brian G Getman, Kofi Adragni, Lisa M Broad, Helene E Sanger, Daniel Ursu, John T Catlow, Steven Swanson, Bryan G Johnson, David B Shaw, David L McKinzie, Junliang Hao
Multiple therapeutic opportunities have been suggested for compounds capable of selective activation of metabotropic glutamate 3 (mGlu3) receptors, but small molecule tools are lacking. As part of our ongoing efforts to identify potent, selective and systemically bioavailable agonists for mGlu2 and mGlu3 receptor subtypes, a series of C4β-N-linked variants of (1S,2S,5R,6S)-2-amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid 1 (LY354740) were prepared and evaluated for both mGlu2 and mGlu3 receptor binding affinity and functional cellular responses...
January 19, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29348321/lower-limbic-metabotropic-glutamate-receptor-5-availability-in-alcohol-dependence
#2
Gil Leurquin-Sterk, Jenny Ceccarini, Cleo L Crunelle, Bart de Laat, Jef Verbeek, Stephanie Deman, Hugo Neels, Guy Bormans, Hendrik Peuskens, Koen Van Laere
Animal studies suggest an important role for the metabotropic glutamate receptor subtype 5 (mGlu5) in the pathophysiology of alcohol dependence, but direct human evidence is lacking. The goal of this study was to investigate cerebral mGlu5 availability in alcohol-dependent patients versus controls using 18F-FPEB positron emission tomography. Methods: Dynamic 90 minute 18F-FPEB scans combined with arterial blood sampling were acquired in 16 recently abstinent alcohol-dependent patients and 32 age-matched controls...
January 18, 2018: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/29346767/functional-principles-of-posterior-septal-inputs-to-the-medial-habenula
#3
Yo Otsu, Salvatore Lecca, Katarzyna Pietrajtis, Charly Vincent Rousseau, Païkan Marcaggi, Guillaume Pierre Dugué, Caroline Mailhes-Hamon, Manuel Mameli, Marco Alberto Diana
The medial habenula (MHb) is an epithalamic hub contributing to expression and extinction of aversive states by bridging forebrain areas and midbrain monoaminergic centers. Although contradictory information exists regarding their synaptic properties, the physiology of the excitatory inputs to the MHb from the posterior septum remains elusive. Here, combining optogenetics-based mapping with ex vivo and in vivo physiology, we examine the synaptic properties of posterior septal afferents to the MHb and how they influence behavior...
January 16, 2018: Cell Reports
https://www.readbyqxmd.com/read/29339723/fasoracetam-in-adolescents-with-adhd-and-glutamatergic-gene-network-variants-disrupting-mglur-neurotransmitter-signaling
#4
Josephine Elia, Grace Ungal, Charlly Kao, Alexander Ambrosini, Nilsa De Jesus-Rosario, Lene Larsen, Rosetta Chiavacci, Tiancheng Wang, Christine Kurian, Kanani Titchen, Brian Sykes, Sharon Hwang, Bhumi Kumar, Jacqueline Potts, Joshua Davis, Jeffrey Malatack, Emma Slattery, Ganesh Moorthy, Athena Zuppa, Andrew Weller, Enda Byrne, Yun R Li, Walter K Kraft, Hakon Hakonarson
The glutamatergic neurotransmitter system may play an important role in attention-deficit hyperactivity disorder (ADHD). This 5-week, open-label, single-blind, placebo-controlled study reports the safety, pharmacokinetics and responsiveness of the metabotropic glutamate receptor (mGluR) activator fasoracetam (NFC-1), in 30 adolescents, age 12-17 years with ADHD, harboring mutations in mGluR network genes. Mutation status was double-blinded. A single-dose pharmacokinetic profiling from 50-800 mg was followed by a single-blind placebo at week 1 and subsequent symptom-driven dose advancement up to 400 mg BID for 4 weeks...
January 16, 2018: Nature Communications
https://www.readbyqxmd.com/read/29339716/to-explore-the-mechanism-of-the-grm4-gene-in-osteosarcoma-by-rna-sequencing-and-bioinformatics-approach
#5
Yunguo Pang, Jinmin Zhao, Mitra Fowdur, Yun Liu, Hao Wu, Maolin He
BACKGROUND Glutamate metabotropic receptor 4 (GRM4) has been correlated with the pathogenesis of osteosarcoma. The objective of this study was to explore the underlying molecular mechanism of GRM4 in osteosarcoma. MATERIAL AND METHODS The expression levels of GRM4 in four human osteosarcoma cell lines and hFOB1.19 cells were examined by real-time quantitative PCR (RT-qPCR). The U2OS cells of the highest GRM4 expression were transfected with lentivirus-mediated small interfering RNA (siRNA). The differentially expressed genes (DEGs) after GRM4 gene silencing were screened through RNA sequencing, and analyzed by bioinformatics...
January 17, 2018: Medical Science Monitor Basic Research
https://www.readbyqxmd.com/read/29337350/alterations-in-mglu5-receptor-expression-and-function-in-the-striatum-in-a-rat-depression-model
#6
Li-Min Mao, John Q Wang
Major depressive disorder is a common form of mental illness. Many brain regions are implicated in the pathophysiology and symptomatology of depression. Among key brain areas is the striatum that controls reward and mood and is involved in the development of core depression-like behavior in animal models of depression. While molecular mechanisms in this region underlying depression-related behavior are poorly understood, the glutamatergic input to the striatum is believed to play a role. In this study, we investigated changes in metabotropic glutamate (mGlu) receptor expression and signaling in the striatum of adult rats in response to prolonged (10-12 weeks) social isolation, a pre-validated animal paradigm modeling depression in adulthood...
January 16, 2018: Journal of Neurochemistry
https://www.readbyqxmd.com/read/29324247/mglu5-dependent-modulation-of-anxiety-during-early-withdrawal-from-binge-drinking-in-adult-and-adolescent-male-mice
#7
Kaziya M Lee, Michal A Coelho, MacKayla A Class, Karen K Szumlinski
Binge alcohol-drinking elicits symptoms of negative affect such as anxiety upon cessation, which is a source of negative reinforcement for perpetuating this pattern of alcohol abuse. Binge-induced anxiety during early (24 h) withdrawal is associated with increased expression of metabotropic glutamate receptor 5 (mGlu5) within the nucleus accumbens shell (AcbSh) of adult male mice, but was unchanged in anxiety-resilient adolescents. Herein, we determined the role of mGlu5 signaling in withdrawal-induced anxiety via pharmacological manipulation using the mGlu5 negative allosteric modulator MTEP and the positive allosteric modulator CDPPB...
January 5, 2018: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/29322377/s-ketamine-current-trends-in-emergency-and-intensive-care-medicine
#8
REVIEW
Helmut Trimmel, Raimund Helbok, Thomas Staudinger, Wolfgang Jaksch, Brigitte Messerer, Herbert Schöchl, Rudolf Likar
S(+)-ketamine, the pure dextrorotatory enantiomer of ketamine has been available for clinical use in analgesia and anesthesia for more than 25 years. The main effects are mediated by non-competitive inhibition of the N-methyl-D-aspartate (NMDA) receptor but S(+)-ketamine also interacts with opioid receptors, monoamine receptors, adenosine receptors and other purinergic receptors. Effects on α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors, metabotropic glutamate receptors (mGluR) and L‑type calcium chanels have also been described...
January 10, 2018: Wiener Klinische Wochenschrift
https://www.readbyqxmd.com/read/29320397/in-silico-analysis-of-the-association-relationship-between-neuroprotection-and-flavors-of-traditional-chinese-medicine-based-on-the-mglurs
#9
Xu Zhang, Liansheng Qiao, Yankun Chen, Bowen Zhao, Yu Gu, Xiaoqian Huo, Yanling Zhang, Gongyu Li
The metabotropic glutamate receptors (mGluRs) are known as both synaptic receptors and taste receptors. This feature is highly similar to the Property and Flavor theory of Traditional Chinese medicine (TCM), which has the pharmacological effect and flavor. In this study, six ligand based pharmacophore (LBP) models, seven homology modeling models, and fourteen molecular docking models of mGluRs were built based on orthosteric and allosteric sites to screening potential compounds from Traditional Chinese Medicine Database (TCMD)...
January 10, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29317611/metabotropic-glutamate-receptor-5-binding-in-male-patients-with-alcohol-use-disorder
#10
Funda Akkus, Yoan Mihov, Valerie Treyer, Simon M Ametamey, Anass Johayem, Smeralda Senn, Susanne Rösner, Alfred Buck, Gregor Hasler
Glutamate signaling plays a major role in addiction. Preclinical research strongly suggests an implication of G-protein-coupled metabotropic glutamate receptor subtype 5 (mGluR5) in nicotine addiction and alcohol use disorder. In humans, smoking is related to a global reduction in mGluR5 availability. In the present study, we investigated mGluR5 in vivo in patients with alcohol use disorder without the confounding effects of smoking. A total of 14 male subjects with alcohol use disorder and at least a 25-day abstinence and 14 matched male non-smoking healthy controls were included in the study...
January 10, 2018: Translational Psychiatry
https://www.readbyqxmd.com/read/29315577/bidirectional-variation-in-glutamate-efflux-in-the-medial-prefrontal-cortex-induced-by-selective-positive-and-negative-allosteric-mglur5-modulators
#11
Sarah N Isherwood, Trevor W Robbins, Jeffrey W Dalley, Anton Pekcec
Dysregulation of prefrontal cortical glutamatergic signalling via NMDA receptor hypofunction has been implicated in cognitive dysfunction and impaired inhibitory control in such neuropsychiatric disorders as schizophrenia, attention deficit hyperactivity disorder and drug addiction. Although NMDA receptors functionally interact with metabotropic glutamate receptor 5 (mGluR5), the consequence of this interaction for glutamate release in the prefrontal cortex (PFC) is unknown. We therefore investigated the effects of positive and negative allosteric mGluR5 modulation on changes in extracellular glutamate efflux in the medial PFC (mPFC) induced by systemic administration of the non-competitive NMDA receptor antagonist dizocilpine (or MK801) in rats...
January 6, 2018: Journal of Neurochemistry
https://www.readbyqxmd.com/read/29301614/metabotropic-glutamate-receptors-2-and-3-as-targets-for-treating-nicotine-addiction
#12
REVIEW
Alan J Cross, Robert Anthenelli, Xia Li
Tobacco smoking, driven by the addictive properties of nicotine, continues to be a worldwide health problem. Based on the well-established role of glutamatergic neurotransmission in drug addiction, novel medication development strategies seek to halt nicotine consumption and prevent relapse to tobacco smoking by modulating glutamate transmission. The presynaptic inhibitory metabotropic glutamate receptors 2 and 3 (mGluR2/3) are key autoreceptors on glutamatergic terminals that maintain glutamate homeostasis...
November 21, 2017: Biological Psychiatry
https://www.readbyqxmd.com/read/29301063/aberrant-epigenetic-gene-regulation-in-gabaergic-interneuron-subpopulations-in-the-hippocampal-dentate-gyrus-of-mouse-offspring-following-developmental-exposure-to-hexachlorophene
#13
Yousuke Watanabe, Hajime Abe, Kota Nakajima, Maky Ideta-Otsuka, Katsuhide Igarashi, Gye-Hyeong Woo, Toshinori Yoshida, Makoto Shibutani
Maternal hexachlorophene (HCP) exposure causes transient disruption of hippocampal neurogenesis in mouse offspring. We examined epigenetically hypermethylated and downregulated genes related to this HCP-induced disrupted neurogenesis. Mated female mice were dietary exposed to 0 or 100 ppm HCP from gestational day 6 to postnatal day (PND) 21 on weaning. The hippocampal dentate gyrus of male offspring was subjected to methyl-capture sequencing and real-time reverse transcription-PCR analyses on PND 21. Validation analyses on methylation identified three genes, Dlx4, Dmrt1, and Plcb4, showing promoter-region hypermethylation...
January 2, 2018: Toxicological Sciences: An Official Journal of the Society of Toxicology
https://www.readbyqxmd.com/read/29286078/direct-binding-of-toll-like-receptor-4-to-ionotropic-glutamate-receptor-n-methyl-d-aspartate-subunit-1-induced-by-lipopolysaccharide-in-microglial-cells-n9-and-eoc-20
#14
Jie Cui, Siyuan Yu, Yihui Li, Pan Li, Feng Liu
Microglia, the primary immune cells in the brain, are the predominant cells regulating inflammation-mediated neuronal damage. In response to immunological challenges, such as lipopolysaccharide (LPS), microglia are activated and the inflammatory process is subsequently initiated. The aim of the present study was to determine whether LPS induces interactions between the Toll-like receptor 4 (TLR4) and the ionotropic glutamate receptor N-methyl-D‑aspartate subunit 1 (GluN1) in N9 and EOC 20 microglial cells...
December 19, 2017: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/29280965/the-glutamatergic-system-in-primary-somatosensory-neurons-and-its-involvement-in-sensory-input-dependent-plasticity
#15
REVIEW
Julia Fernández-Montoya, Carlos Avendaño, Pilar Negredo
Glutamate is the most common neurotransmitter in both the central and the peripheral nervous system. Glutamate is present in all types of neurons in sensory ganglia, and is released not only from their peripheral and central axon terminals but also from their cell bodies. Consistently, these neurons express ionotropic and metabotropic receptors, as well as other molecules involved in the synthesis, transport and release of the neurotransmitter. Primary sensory neurons are the first neurons in the sensory channels, which receive information from the periphery, and are thus key players in the sensory transduction and in the transmission of this information to higher centers in the pathway...
December 27, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29278824/metabotropic-glutamate-receptors-the-potential-for-therapeutic-applications-in-alzheimer-s-disease
#16
REVIEW
Filippo Caraci, Ferdinando Nicoletti, Agata Copani
A dysfunction of glutamate signaling is implicated at several levels in the pathogenesis of Alzheimer's disease. Currently, metabotropic glutamate receptors, which have a wide distribution in the central nervous system and activate a multitude of cell signaling pathways, are pursued as targets for therapeutic intervention in Alzheimer's disease. Research is still limited, but results underscore the relevance of ongoing studies. Here we discuss the latest updates regarding metabotropic glutamate receptors and their role in Alzheimer's disease, as well as promising metabotropic glutamate receptor ligands that have been investigated in preclinical models of Alzheimer's disease...
December 23, 2017: Current Opinion in Pharmacology
https://www.readbyqxmd.com/read/29275640/lost-in-translation-a-critical-look-at-the-role-that-animal-models-of-obsessive-compulsive-disorder-play-in-current-drug-discovery-strategies
#17
Kurt Leroy Hoffman, Hugo Cano-Ramírez
Obsessive-compulsive disorder (OCD) is a severe neuropsychiatric illness estimated to affect between 1-3% of the population. In today's literature, there are a number well-validated and convincing animal models of OCD described. Areas covered: Herein, the authors look at the role that animal models of OCD (including transgenic models, deer mouse stereotypy, quinpirole sensitization, post-training signal attenuation, and mouse marble burying) have played in determining the current directions of OCD drug discovery...
December 23, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/29262299/atpase-n-ethylmaleimide-sensitive-fusion-protein-a-novel-key-player-for-causing-spontaneous-network-excitation-in-human-temporal-lobe-epilepsy
#18
Christina Herold, Hans-Jürgen Bidmon, Heinz W Pannek, Volkmar Hans, Ali Gorji, Erwin-Josef Speckmann, Karl Zilles
The molecular basis for onset, maintenance and propagation of excitation along neuronal networks in epilepsy is still poorly understood. Beside different neurotransmitter receptors that control signal transfer at the synapse, one key regulator involved in all of these processes is the ATPase N-ethylmaleimide-sensitive fusion protein (NSF). Therefore, we analyzed receptor subunits and NSF levels in tissues from the medial temporal gyrus of patients with pharmaco-resistant focal temporal lobe epilepsy resected during epilepsy surgery and autopsy controls...
December 17, 2017: Neuroscience
https://www.readbyqxmd.com/read/29259100/mglur5-antagonism-increases-autophagy-and-prevents-disease-progression-in-the-zq175-mouse-model-of-huntington-s-disease
#19
Khaled S Abd-Elrahman, Alison Hamilton, Shaunessy R Hutchinson, Fang Liu, Ryan C Russell, Stephen S G Ferguson
Huntington's disease (HD) is a neurodegenerative disease caused by an expansion in the huntingtin protein (also called Htt) that induces neuronal cell death with age. We found that the treatment of 12-month-old symptomatic heterozygous and homozygous zQ175 huntingtin knockin mice for 12 weeks with CTEP, a negative allosteric modulator of metabotropic glutamate receptor 5 (mGluR5), reduced the size and number of huntingtin aggregates, attenuated caspase-3 activity, and reduced both neuronal apoptosis and neuronal loss in brain tissue...
December 19, 2017: Science Signaling
https://www.readbyqxmd.com/read/29258835/the-glun1-glun2b-nmda-receptor-and-metabotropic-glutamate-receptor-1-negative-allosteric-modulator-has-enhanced-neuroprotection-in-a-rat-subarachnoid-hemorrhage-model
#20
Zongyong Zhang, Junke Liu, Cundong Fan, Leilei Mao, Rongxia Xie, Suyun Wang, Mingfeng Yang, Hui Yuan, Xiaoyi Yang, Jingyi Sun, Jian Wang, Jiming Kong, Siluo Huang, Baoliang Sun
Excessive glutamate in cerebrospinal fluid after subarachnoid hemorrhage (SAH) causes excitotoxic damage through calcium overloading and a subsequent apoptotic cascade. GluN1/GluN2B containing N-methyl-Daspartate (NMDA) receptor and metabotropic glutamate receptor 1 (mGluR1) can play a leading role in glutamate-mediated excitotoxicity. Here we report that Ifenprodil (100μM), a negative allosteric modulator (NAM) of GluN1/GluN2B NMDA receptors, and JNJ16259685 (10μM), a NAM of mGluR1, have an additive efficacy against glutamate (100μM)-induced Ca2+ release and cell apoptosis in primary cortical, hippocampal, and cerebellar granule neurons...
December 16, 2017: Experimental Neurology
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