Metabotropic Glutamate Receptor
The Role of Ca2+/Calmodulin Dependent Protein Kinase II Alpha in Group 1 Metabotropic Glutamate Receptor Endocytosis and Signalling
... CaMKII is a well-established player in some processes that contribute to learning and memory. For example, CaMKII is required and sufficient for LTP induction and spatial learning tasks. CaMKIIα mutant mice were impaired ...
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Involvement of metabotropic glutamate receptor 5, AKT/PI3K Signaling and NF-κB pathway in methamphetamine-mediated increase in IL-6 and IL-8 expression in astrocytes
... the receptor involved in mediating this ...of metabotropic gluta- mate receptors in MA-mediated neurotoxicity and/or cog- nitive impairment ...the metabotropic glutamate receptor-5 ...
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Group I metabotropic glutamate receptor mediated dynamic immune dysfunction in children with fragile X syndrome
... mGluR: metabotropic glutamate receptor; MPEP: 2-methyl-6-(phenylethynyl) pyridine hydrochloride; MTEP: 3-((2-methyl-1,3-thiazol-4-yl)ethynyl)pyridine hydrochloride; NF κ B: nuclear factor kappa beta; ...
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Opioid antinociception and antihyperalgesia in combination with metabotropic glutamate receptor antagonism
... the metabotropic class of glutamate receptors is particularly interesting in this ...The metabotropic glutamate receptor subtypes 1 (mGluR1) and 5 (mGluR5) are post-synaptic receptors ...
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Association of metabotropic glutamate receptor 3 gene polymorphisms with schizophrenia risk: evidence from a meta-analysis
... of metabotropic glutamate receptor 3 (GRM3) rs274622, rs1468412, rs917071, rs6465084, and rs2299225 polymorphisms in schizophrenia remains ...
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Covalent Allosteric Probe for the Metabotropic Glutamate Receptor 2: Design, Synthesis, and Pharmacological Characterization
... (9) Monn, J. A.; Prieto, L.; Taboada, L.; Pedregal, C.; Hao, J.; Reinhard, M. R.; Henry, S. S.; Goldsmith, P. J.; Beadle, C. D.; Walton, L.; Man, T.; Rudyk, H.; Clark, B.; Tupper, D.; Baker, S. R.; Lamas, C.; Montero, ...
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Discovery and Kinetic Profiling of 7-Aryl-1,2,4-triazolo[4,3-a]pyridines: Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 2
... To understand more about the key in vitro parameters that could drive in vivo efficacy, we have focused on the ligand binding kinetics in addition to more classical in vitro parameters. It is now becoming increasingly ...
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Pyk2 uncouples metabotropic glutamate receptor G protein signaling but facilitates ERK1/2 activation
... while facilitating ERK1/2 phosphorylation. The direct association of Pyk2 with mGluR1a appears to coordinate the formation of a protein complex that includes Src bound to Pyk2 and potentially calmodulin bound to the ...
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Intracellular Ca2+ release mediated by metabotropic glutamate receptor activation in the leech giant glial cell
... hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA)/kainate receptors by reference to their artificial agonists (Nakanishi, 1992; Watkins et al. 1990). Metabotropic glutamate receptors (mGluRs) are coupled to ...
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11C-LY2428703, a positron emission tomographic radioligand for the metabotropic glutamate receptor 1, is unsuitable for imaging in monkey and human brains
... We also ex- amined factors known to affect the utility of radioligands for brain imaging: blockade of entry into brain by efflux transporters at the blood – brain barrier, the density of[r] ...
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Regulation of Akt and Wnt signalling by the dopamine D2 receptor and metabotropic glutamate receptor 2/3
... Wnt proteins are secreted glycoproteins that bind to Frizzled (Fz) receptors and the co-receptor low-density lipoprotein receptor-related protein 5/6 (LRP5/6). This event can activate one or more of the 3 ...
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Is metabotropic glutamate receptor 5 upregulated in prefrontal cortex in fragile X syndrome?
... binding curves best fit the one-site homologous model, which was used to determine binding measures. The mGluR5 receptor density increased with marginal sig- nificance (+16%; t = 1.97, df = 29, P = 0.058) for FXS ...
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Metabotropic glutamate receptor mediated modulation of N-methyl-D-aspartate (NMDA) receptor-channels in the rat hippocampus
... A great deal of attention has focused on protein kinase C (PKC) as a modulator of NMDA mediated responses due to its abundance in the CNS (Brandt, et aL, 1987) and also its ability to readily phosphorylate other ion ...
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Impact of allosteric modulation: exploring the binding kinetics of glutamate and other orthosteric ligands of the metabotropic glutamate receptor 2
... of glutamate, LY354740 or LY341495, which shows that the presence of the NAM does not inhibit the orthosteric agonists and antagonist from binding to the ...
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Constitutive activity of the metabotropic glutamate receptor 2 explored with a whole-cell label-free biosensor
... 10% receptor activation. Blockade of glutamate binding may thus increase the agonist-induced response by a similar ...the receptor is constitutively active and that LY341495 is behaving as an inverse ...
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Regulation of Metabotropic Glutamate Receptor 5 activity by Ca2+/Calmodulin-dependent Protein Kinase IIα
... stores (Dhami and Ferguson, 2006). CaMKIIα was previously found to desensitize mGluR1-mediated IP formation in striatal neurons (Jin et al., 2013a). Therefore, we examined whether GFP-CaMKIIα overexpression leads to an ...
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Metabotropic glutamate receptor 5 may be involved in macrophage plasticity
... of glutamate in the macrophages, maintaining the high glutamate gradient across the intra- and extra- cellular ...of glutamate, the cystine/glutamate antiporter functions in reverse, taking up ...
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Rethinking metabotropic glutamate receptor 5 pathological findings in psychiatric disorders: implications for the future of novel therapeutics
... Discussion: The majority of studies in the schizophrenia post-mortem brain indicate that total mGluR5 expression is unaltered. However, close examination of the literature suggests that these findings are superficial, ...
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The metabotropic glutamate receptor 5 role on motor behavior involves specific neural substrates
... NMDA receptor antagonist, MK801, into the ventral and dorsal hippocampus promotes in- creased locomotor activity in the open field apparatus, al- though the increase promoted by dorsal hippocampus MK801 infusion ...
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Metabotropic glutamate receptor 5 knockout reduces cognitive impairment and pathogenesis in a mouse model of Alzheimer's disease
... Given the potential role for mGluR5 as a receptor for Aβ [17-20], we crossed mGluR5 knockout mice with APPswe/ PS1ΔE9 mice. The double transgenic APPswe/PS1ΔE9 mice were previously found to exhibit impaired cogni- ...
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