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Metabotropic glutamate receptor

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https://www.readbyqxmd.com/read/28109949/positional-isomers-of-bispyridine-benzene-derivatives-induce-efficacy-changes-on-mglu5-negative-allosteric-modulation
#1
Xavier Gómez-Santacana, James A R Dalton, Xavier Rovira, Jean Philippe Pin, Cyril Goudet, Pau Gorostiza, Jesús Giraldo, Amadeu Llebaria
Modulation of metabotropic glutamate receptor 5 (mGlu5) with partial allosteric antagonists has received increased interest due to their favourable in vivo activity profiles compared to the unfavourable side-effects of full inverse agonists. Here we report on a series of bispyridine benzene derivatives with a functional molecular switch affecting antagonistic efficacy, shifting from inverse agonism to partial antagonism with only a single change in the substitution pattern of the benzene ring. These efficacy changes are explained through computational docking, revealing two different receptor conformations of different energetic stability and different positional isomer binding preferences...
January 12, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28108498/mglur2-versus-mglur3-metabotropic-glutamate-receptors-in-primate-dorsolateral-prefrontal-cortex-postsynaptic-mglur3-strengthen-working-memory-networks
#2
Lu E Jin, Min Wang, Veronica C Galvin, Taber C Lightbourne, Peter Jeffrey Conn, Amy F T Arnsten, Constantinos D Paspalas
The newly evolved circuits in layer III of primate dorsolateral prefrontal cortex (dlPFC) generate the neural representations that subserve working memory. These circuits are weakened by increased cAMP-K(+) channel signaling, and are a focus of pathology in schizophrenia, aging, and Alzheimer's disease. Cognitive deficits in these disorders are increasingly associated with insults to mGluR3 metabotropic glutamate receptors, while reductions in mGluR2 appear protective. This has been perplexing, as mGluR3 has been considered glial receptors, and mGluR2 and mGluR3 have been thought to have similar functions, reducing glutamate transmission...
January 19, 2017: Cerebral Cortex
https://www.readbyqxmd.com/read/28104407/metabotropic-glutamate-and-gaba-receptors-modulate-cellular-excitability-and-glutamatergic-transmission-in-chicken-cochlear-nucleus-angularis-neurons
#3
Wei Shi, Yong Lu
Neurons in the avian cochlear nucleus angularis (NA) receive glutamatergic input from the auditory nerve, and GABAergic input from the superior olivary nucleus. Physiologically heterogeneous, NA neurons perform multiple functions including encoding sound intensity information. Using in vitro whole-cell patch recordings from acute brain slices and immunohistochemistry staining, we investigated neuromodulation mediated by metabotropic glutamate and GABA receptors (mGluRs and GABABRs) in NA neurons. Based on their intrinsic firing patterns in response to somatic current injections, NA neurons were classified into one-spike (onset), damped, and tonic cells...
January 16, 2017: Hearing Research
https://www.readbyqxmd.com/read/28100750/target-dependent-compartmentalization-of-the-corelease-of-glutamate-and-gaba-from-the-mossy-fibers
#4
Emilio J Galván, Rafael Gutiérrez
: The mossy fibers (MFs) corelease glutamate and GABA onto pyramidal cells of CA3 during development, until the end of the third postnatal week. However, the major target cells of the MF are the interneurons of CA3. Therefore, it has been shown that the interneurons of the hilus and stratum lucidum receive this dual monosynaptic input on MF stimulation. Because the plasticity of glutamatergic transmission from the different terminals of the MF is target specific, we here asked whether the corelease of glutamate and GABA was also subjected to a target-dependent compartmentalization...
January 18, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28096465/sequences-within-the-c-terminus-of-the-metabotropic-glutamate-receptor-mglur5-are-responsible-for-inner-nuclear-membrane-localization
#5
Ismail Sergin, Yuh-Jiin I Jong, Steven K Harmon, Vikas Kumar, Karen L O'Malley
Traditionally G-protein coupled receptors (GPCR) are thought to be located on the cell surface where they transmit extracellular signals to the cytoplasm. However recent studies indicate that some GPCRs are also localized to various subcellular compartments such as the nucleus where they appear required for various biological functions. For example, the metabotropic glutamate receptor 5, mGluR5, is concentrated at the inner nuclear membrane (INM) where it mediates Ca2+ changes in the nucleoplasm by coupling with Gq/11...
January 17, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28088471/effects-of-group-i-metabotropic-glutamate-receptor-antagonists-on-sensitivity-to-reinforcer-magnitude-and-delayed-reinforcement-in-a-delay-discounting-task-in-rats-contribution-of-delay-presentation-order
#6
Justin R Yates, Katherine K Rogers, Benjamin T Gunkel, Nicholas A Prior, Mallory N Hughes, Sara M Sharpe, Hunter L Campbell, Anthony B Johnson, Margaret G Keller, Kerry A Breitenstein, Hansen N Shults
Metabotropic glutamate receptor 1 (mGluR1) blockade has been shown to decrease impulsive choice, as measured in delay discounting. However, several variables are known to influence an animal's discounting, including sensitivity to delayed reinforcement and sensitivity to reinforcer magnitude. The goal of this experiment was to determine the effects of mGluR1, as well as mGluR5, antagonism on these parameters. Forty Sprague Dawley rats were trained in delay discounting, in which consistently choosing a small, immediate reward reflects impulsive choice...
January 12, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28074469/development-of-cone-photoreceptors-and-their-synapses-in-the-human-and-monkey-fovea
#7
Anita Hendrickson, Chi Zhang
During retinal development, ribbon synapse assembly in the photoreceptors is a crucial step involving numerous molecules. While the developmental sequence of plexiform layers in human retina has been characterized, the molecular steps of synaptogenesis remain largely unknown. In the present study, we focused on the central rod-free region of primate retina, the fovea, to specifically investigate the development of cone photoreceptor ribbon synapses. Immunocytochemistry and electron microscopy were utilized to track the expression of photoreceptor transduction proteins and ribbon and synaptic markers in fetal human and Macaca retina...
January 11, 2017: Journal of Comparative Neurology
https://www.readbyqxmd.com/read/28067903/modulation-of-excitation-on-parvalbumin-interneurons-by-neuroligin-3-regulates-the-hippocampal-network
#8
Jai S Polepalli, Hemmings Wu, Debanjan Goswami, Casey H Halpern, Thomas C Südhof, Robert C Malenka
Hippocampal network activity is generated by a complex interplay between excitatory pyramidal cells and inhibitory interneurons. Although much is known about the molecular properties of excitatory synapses on pyramidal cells, comparatively little is known about excitatory synapses on interneurons. Here we show that conditional deletion of the postsynaptic cell adhesion molecule neuroligin-3 in parvalbumin interneurons causes a decrease in NMDA-receptor-mediated postsynaptic currents and an increase in presynaptic glutamate release probability by selectively impairing the inhibition of glutamate release by presynaptic Group III metabotropic glutamate receptors...
January 9, 2017: Nature Neuroscience
https://www.readbyqxmd.com/read/28064424/gender-related-hippocampal-proteomics-study-from-young-rats-after-chronic-unpredicted-mild-stress-exposure
#9
Lin-Na Ning, Teng Zhang, Jiang Chu, Na Qu, Li Lin, Ying-Yan Fang, Yan Shi, Peng Zeng, Er-Li Cai, Xiao-Ming Wang, Qun Wang, You-Ming Lu, Xin-Wen Zhou, Qi Zhang, Qing Tian
Clinical data have shown women are more susceptible to depression. This study was performed to identify differentially regulated proteins from hippocampus in chronic unpredicted mild stress (CUMS)-exposed male and female young rats. After 7 weeks of CUMS, depressed male (M-D) and female rats (F-D) and unstressed male (M-C) and female controls (F-C) were studied. By proteomics analysis, 74 differential proteins in F-C/M-C, 79 in F-D/M-D, 77 in F-D/F-C, and 32 in M-D/M-C were found. Further, the synapse-related proteins, cytoskeleton protein tau, and stress-related kinases in hippocampus were assayed by Western blotting...
January 7, 2017: Molecular Neurobiology
https://www.readbyqxmd.com/read/28063803/tamoxifen-and-ici-182-780-activate-hypothalamic-g-protein-coupled-estrogen-receptor-1-to-rapidly-facilitate-lordosis-in-female-rats
#10
Nathan Long, Bertha Long, Asma Mana, Dream Le, Lam Nguyen, Sima Chokr, Kevin Sinchak
In the female rat, sexual receptivity (lordosis) can be facilitated by sequential activation of estrogen receptor (ER) α and G protein-coupled estrogen receptor 1 (GPER) by estradiol. In the estradiol benzoate (EB) primed ovariectomized (OVX) rat, EB initially binds to ERα in the plasma membrane that complexes with and transactivates metabotropic glutamate receptor 1a to activate β-endorphin neurons in the arcuate nucleus of the hypothalamus (ARH) that project to the medial preoptic nucleus (MPN). This activates MPN μ-opioid receptors (MOP), inhibiting lordosis...
January 4, 2017: Hormones and Behavior
https://www.readbyqxmd.com/read/28049619/synthesis-and-evaluation-of-1-cyclopropylmethyl-4-4-11-c-methoxyphenyl-piperidin-1-yl-2-oxo-1-2-dihydropyridine-3-carbonitrile-11-c-cmdc-for-pet-imaging-of-metabotropic-glutamate-receptor-2-in-the-rat-brain
#11
Yufei Ma, Katsushi Kumata, Joji Yui, Yiding Zhang, Tomoteru Yamasaki, Akiko Hatori, Masayuki Fujinaga, Nobuki Nengaki, Lin Xie, Hui Wang, Ming-Rong Zhang
Brain metabotropic glutamate receptor 2 (mGluR2) has been proposed as a therapeutic target for the treatment of schizophrenia-like symptoms arising from increased glutamate transmission in the forebrain. However, there does not exist a reliable tool for the study of mGluR2 in human neuroimaging. The purpose of this study was to radiosynthesize 1-(cyclopropylmethyl)-4-(4-[(11)C]methoxyphenyl)piperidin-1-yl-2-oxo-1,2-dihydropyridine-3-carbonitrile ([(11)C]CMDC) and evaluate its potential as a positron emission tomography (PET) radiotracer for imaging mGluR2 in the rat brain...
December 23, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28039371/granular-layer-neurons-control-cerebellar-neurovascular-coupling-through-an-nmda-receptor-no-dependent-system
#12
Lisa Mapelli, Giuseppe Gagliano, Teresa Soda, Umberto Laforenza, Francesco Moccia, Egidio D'Angelo
: Neurovascular coupling (NVC) is the process whereby neuronal activity controls blood vessel diameter. In the cerebellum, the molecular layer is regarded as the main NVC determinant. However, the granular layer is a region with variable metabolic demand caused by large activity fluctuations, that shows a prominent expression of NMDA receptors (NMDARs) and nitric oxide synthase (NOS) and is therefore much more suitable for effective NVC. Here we show that, in the granular layer of acute rat cerebellar slices, capillary diameter rapidly changes following mossy fiber stimulation...
December 30, 2016: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28030475/spinal-intracellular-metabotropic-glutamate-receptor-5-mglur5-contributes-to-pain-and-c-fos-expression-in-a-rat-model-of-inflammatory-pain
#13
Kathleen Vincent, Shu Fan Wang, André Laferrière, Naresh Kumar, Terence J Coderre
Metabotropic glutamate receptor 5 (mGluR5) is an excitatory G-protein coupled receptor present in the spinal cord dorsal horn (SCDH) where it has a well-established role in pain. In addition to its traditional location on the cytoplasmic membrane, recent evidence shows that these receptors are present intracellularly on the nuclear membrane in the SCDH and are implicated in neuropathic pain. Nuclear mGluR5 is a functional receptor that binds glutamate entering the cell through the neuronal glutamate transporter (GT) EAAT3 and activates transcription factor c-fos, whereas plasma membrane mGluR5 is responsible for c-jun activation...
December 26, 2016: Pain
https://www.readbyqxmd.com/read/28028604/molecular-mechanisms-of-group-i-metabotropic-glutamate-receptor-mediated-ltp-and-ltd-in-basolateral-amygdala-in-vitro
#14
A Chen, W W Hu, X L Jiang, M Potegal, H Li
The roles of group I metabotropic glutamate receptors, metabotropic glutamate receptor 1 (mGluR1) and mGluR5, in regulating synaptic plasticity and metaplasticity in the basolateral amygdala (BLA) remain unclear. The present study examined mGluR1- and mGluR5-mediated synaptic plasticity in the BLA and their respective signaling mechanisms. Bath application of the group I mGluR agonist, 3,5-dihydroxyphenylglycine (DHPG) (20 μM), directly suppressed basal fEPSPs (84.5 ± 6.3% of the baseline). The suppressive effect persisted for at least 30 min after washout; it was abolished by the mGluR1 antagonist 7-(hydroxyimino)cyclopropa[b]chromen-1a-carboxylate ethyl ester (CPCCOEt) but was unaffected by the mGluR5 antagonist 2-methyl-6- (phenylethynyl)-pyridine (MPEP)...
December 28, 2016: Psychopharmacology
https://www.readbyqxmd.com/read/28019025/mtep-impedes-the-neuronal-polarization-and-the-activity-of-the-akt-nf-%C3%AE%C2%BAb-pathway-in-rat-hippocampal-neurons
#15
Xiaohua Zhang, Ming Hu, Lin Zhang, Jing An, Wenhui Yan, Zhichao Zhang, Jianxin Liu, Haixia Lu, Xinlin Chen, Yong Liu
Metabotropic glutamate receptor 5 (mGluR5) is extensively involved in neural survival, differentiation, dendritic morphology, synaptic plasticity, and neural circuit formation. However, little is known about its role in neuronal polarization and axon outgrowth. In this study, we applied the selective agonist (RS)-2-chloro-5-hydroxyphenylglycine sodium salt and antagonist 3-[(2-methyl-4-thaizolyl) ethynyl] pyridine (MTEP) of mGluR5 to the cultured hippocampal neurons to observe the neuronal polarization and axon outgrowth, and further explored the possible intracellular signal transduction pathway...
December 26, 2016: Journal of Neuroscience Research
https://www.readbyqxmd.com/read/28012867/chronic-oral-administration-of-mpep-an-antagonist-of-mglu5-receptor-during-gestation-and-lactation-alters-mglu5-and-a2a-receptors-in-maternal-and-neonatal-brain
#16
Antonio López-Zapata, David Agustín León-Navarro, María Crespo, José Luis Albasanz, Mairena Martín
Antidepressant and anxiolytic drugs are widely consumed even by pregnant and lactating women. The metabotropic glutamate receptor 5 (mGlu5) antagonist 2-methyl-6-(phenylethynyl)-pyridine (MPEP) exerts antidepressant- and anxiolytic-like actions. Given that treatment for anxiety and depression use to be prolonged in time, it is conceivable a possible modulation of metabotropic glutamate receptors (mGlu receptors) after prolonged MPEP exposure, which could also modify adenosine A2A receptors (A2AR) since functional cross-talk between them has been reported...
December 22, 2016: Neuroscience
https://www.readbyqxmd.com/read/28012274/activity-dependent-switch-of-gabaergic-inhibition-into-glutamatergic-excitation-in-astrocyte-neuron-networks
#17
Gertrudis Perea, Ricardo Gómez, Sara Mederos, Ana Covelo, Jesús J Ballesteros, Laura Schlosser, Alicia Hernández-Vivanco, Mario Martín-Fernández, Ruth Quintana, Abdelrahman Rayan, Adolfo Díez, Marco Fuenzalida, Amit Agarwal, Dwight E Bergles, Bernhard Bettler, Denise Manahan-Vaughan, Eduardo D Martín, Frank Kirchhoff, Alfonso Araque
Interneurons are critical for proper neural network function and can activate Ca(2+) signaling in astrocytes. However, the impact of the interneuron-astrocyte signaling into neuronal network operation remains unknown. Using the simplest hippocampal Astrocyte-Neuron network, i.e., GABAergic interneuron, pyramidal neuron, single CA3-CA1 glutamatergic synapse, and astrocytes, we found that interneuron-astrocyte signaling dynamically affected excitatory neurotransmission in an activity- and time-dependent manner, and determined the sign (inhibition vs potentiation) of the GABA-mediated effects...
December 24, 2016: ELife
https://www.readbyqxmd.com/read/28011638/a-critical-role-for-ubiquitination-in-the-endocytosis-of-glutamate-receptors
#18
Ravinder Gulia, Rohan Sharma, Samarjit Bhattacharyya
Group I metabotropic glutamate receptors (mGluRs) play important roles in various neuronal processes and they elicit changes in synaptic efficacy through AMPAR endocytosis. Trafficking of mGluRs plays important roles in controlling the precise localization of these receptors at specific region of the cell as well as it regulates the activity of these receptors. Despite this obvious significance we know very little about the cellular mechanisms that control the trafficking of group I mGluRs. We show here that ligand-mediated internalization of group I mGluRs is ubiquitination dependent...
December 23, 2016: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28008418/regulation-of-group-i-metabotropic-glutamate-receptors-by-mapk-erk-in-neurons
#19
Li-Min Mao, John Q Wang
Group I metabotropic glutamate receptors (mGluR1 and mGluR5 subtypes) are regulated by protein kinases. A recent focus is mitogen-activated protein kinases (MAPK). A prototypic subclass of MAPKs, extracellular signal-regulated kinases (ERK), is densely expressed in adult brain postmitotic neurons. This kinase resides in not only the cytoplasm around the nucleus, also the neuronal peripheral structures such as synapses. Recombinant ERK2 binds to C terminal tails of mGluR1a in vitro and native ERK1/2 forms complexes with mGluR1/5 in neurons in vivo...
2016: Journal of Nature and Science
https://www.readbyqxmd.com/read/28004452/inhibitory-mechanism-of-l-glutamic-acid-on-spawning-of-the-starfish-patiria-asterina-pectinifera
#20
Masatoshi Mita
L-Glutamic acid was previously identified as an inhibitor of spawning in the starfish Patiria (Asterina) pectinifera; this study examined how L-glutamic acid works. Oocyte release from ovaries of P. pectinifera occurred after germinal vesicle breakdown (GVBD) and follicular envelope breakdown (FEBD) when gonads were incubated ex vivo with either relaxin-like gonad-stimulating peptide (RGP) or 1-methyladenine (1-MeAde). L-Glutamic acid blocked this spawning phenotype, causing the mature oocytes to remain within the ovaries...
December 22, 2016: Molecular Reproduction and Development
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