Objective To investigate the effects of group Ⅲ metabotropic glutamate receptors(mGluRs) subtypes on neuropathic pain. (shsmu.edu.cn)
Effects of group Ⅲ metabotropic glutamate receptors subtypes on neuropathic pain[J]. , doi: 10.3969/j.issn.1674-8115.2013.10.003 . (shsmu.edu.cn)
The structures of AMPA receptors in complex with auxiliary proteins are resolved by cryo-electron microscopy, and reveal conformational and permeation pathway changes that are associated with activation and desensitization of ionotropic glutamate receptors. (nature.com)
Neurotransmission in the hippocampus is modulated variously through presynaptic metabotropic glutamate receptors (mGluRs). (elsevierpure.com)
We have determined the role of subgroups of metabotropic glutamate receptors (mGluRs) in the nucleus of the solitary tract (NTS) of normotensive Wistar rats. (elsevierpure.com)
Quisqualic acid is an agonist of the AMPA, kainate, and group I metabotropic glutamate receptors. (wikipedia.org)
L - quisqualic acid is a glutamate receptor agonist, acting at AMPA receptors and metabotropic glutamate receptors positively linked to phosphoinositide hydrolysis. (wikipedia.org)
These data suggest that glutamate, acting at several metabotropic receptors expressed by astrocytes, could modulate glial activity evoked by neurotransmitters and thereby influence the ongoing modulation of neurons by astrocytes. (jneurosci.org)
Acute stress increases glutamate release, membrane trafficking of AMPA and NMDA receptors, and potentially glutamate clearance in the prefrontal cortex through various mechanisms that involve glucocorticoid regulation. (nature.com)
Chronic stress has been associated with a loss of glutamate receptors, impaired glutamate cycling and a suppression of glutamate transmission that may be attributable to the observed impairment of prefrontal cortex-dependent cognitive functions. (nature.com)
Recent studies have shed light on the mechanisms by which stress and glucocorticoids affect glutamate transmission, including effects on glutamate release, glutamate receptors and glutamate clearance and metabolism. (nature.com)
Both of them block NMDA-subtype glutamate receptors. (dr-bob.org)
If we think about some of those novel mechanisms, it would be glutamate-type mechanisms that hit the NMDA [N-methyl-D-aspartate] and the AMPA receptors and the cascade under glutamate, it would be the GABAergictreatment [gamma-aminobutyric acid]options, which would be primarily the neural steroids, which modulate those intrasynaptic, but extrasynaptic GABA receptors. (psychiatrictimes.com)
Tezampanel is an antagonist at the AMPA and kainate families of ionotropic glutamate receptors, with selectivity for the GluR5 subtype of the kainate receptor. (adooq.com)
S)-Glutamic acid acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). (adooq.com)
CNQX is a competitive, non-NMDA glutamate receptor antagonist (IC50s = 0.3 and 1.5 uM for AMPA and kainate receptors, respectively, versus IC50 = 25 uM for NMDA receptors). (adooq.com)
First, it has high affinity: only a small amount of compound is needed to achieve a very large effect on metabotropic glutamate receptors (mGluR). (ub.edu)
There are compounds that affect many subtypes of receptors in the same protein family, and modern pharmacology is looking for compounds that affect only one target, a single type of protein. (ub.edu)
Of the eight subtypes of mGluR receptors, it is specific to mGlu5. (ub.edu)
Metabotropic glutamate (mGlu) receptors, which include mGlu1-8 receptors, are a heterogeneous family of G-protein-coupled receptors which function to modulate brain excitability via presynaptic, postsynaptic and glial mechanisms. (aspetjournals.org)
This suggests that these receptors may have evolved to monitor glutamate that has "spilled" out of the synapse. (aspetjournals.org)
Recent progress on the molecular and pharmacological aspects of these presynaptic mGlu receptors is unveiling their functions and the therapeutic directions of agents designed for these novel glutamate receptor targets. (aspetjournals.org)
Among these diverse features, it should be acknowledged that auto-antibodies toward glutamate receptors, GABA receptors, and K + channel-related proteins are preferentially found in autoimmune limbic encephalitis but not in IMCAs [ 10 ] (Table 1 ). (springer.com)
Radiprodil targets the hyperactive receptors associated with the development and progression of GRIN-related disorders by potently and selectively modulating the Nmethyl-D-aspartate (NMDA) receptor subtype 2B (NR2B). (businesswire.com)
It has been shown to inhibit NMDA glutamate currents when tested using receptors containing NR2B subunits coded by gain of function (GoF) mutations in the GRIN2B and GRIN2A genes, which are known to cause GRIN-related disorders. (businesswire.com)
Atomic structures of the ligand-binding core of the original metabotropic glutamate receptor 1 obtained using X-ray crystallography provide a foundation for determining the initial receptor activation of this important family of G-protein-coupled receptors. (nih.gov)
This thesis explores the dynamic organization of glutamate receptors and membrane lipids in the postsynaptic membrane of neurons. (uu.nl)
Overall, the thesis provides valuable insights into the nanoscale organization of glutamate receptors and membrane lipids in the postsynaptic membrane. (uu.nl)
NMDA receptors are glutamate-gated ion channels. (medlineplus.gov)
NMDA6
Firstly the NMDA receptor antagonists Memantine and NitroMemantine block excessive extrasynaptic glutamate excitation while keeping synaptic transmission therefore limiting excessive calcium influx and JWH 073 production of ROS/RNS. (buyresearchchemicalss.net)
Most of the clinical effects can be explained by the interaction of ethanol with various neurotransmitters and neuroreceptors in the brain, including those interacting with gamma-aminobutyric acid (GABA), glutamate (NMDA), and opiates. (medscape.com)
In particular, the amino acid glutamate has been shown to act as a neurotoxin which exerts its toxic effect on RGCs predominantly through the N-methyl-D-aspartate (NMDA) subtype of glutamate receptor. (nih.gov)
Glutamate stimulates its own release in a positive feedback loop by its interaction with the non-NMDA receptor subtypes. (nih.gov)
Of particular importance for future clinical use of NMDA receptor antagonists in the treatment of acute vascular insults is the finding that some drugs can prevent glutamate-induced neurotoxicity, even when administered a few hours after the onset of retinal ischemia. (nih.gov)
GRIN-related disorders are genetically defined, rare pediatric developmental and epileptic encephalopathies (DEEs) caused by mutations in the gene coding on the NMDA glutamate receptor. (businesswire.com)
AMPA2
Zonampanel (YM 872) is a selective antagonist of the glutamate receptor subtype, α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptor. (adooq.com)
Chapter 5 examines the AMPA receptor, particularly the GluA3-containing subtype. (uu.nl)
Allosteric Modulator2
Radiprodil is an investigational, selective negative allosteric modulator of the Nmethyl-D-aspartate receptor subtype 2B (NR2B). (businesswire.com)
Dipraglurant is a metabotropic glutamate receptor subtype 5 negative allosteric modulator, or mGlu5 NAM. (addexpharma.com)
Metabotropic glutamate5
Although metabotropic glutamate receptor (mGluR) modulation has been studied extensively in neurons, it has not been investigated in astrocytes. (jneurosci.org)
may interact with mGluR1, another group I metabotropic glutamate receptor. (thermofisher.com)
The autoantigens include glutamic acid decarboxylase 65 (GAD65), voltage-gated Ca 2+ channel (VGCC), metabotropic glutamate receptor type 1 (mGluR1), and glutamate receptor delta (GluRdelta). (springer.com)
Chapter 6 focuses on the metabotropic glutamate receptor mGluR5, exploring its distribution and dynamics in relation to the postsynaptic density. (uu.nl)
Fragile X Mental Retardation Protein and Cerebral Expression of Metabotropic Glutamate Receptor Subtype 5 in Men with Fragile X Syndrome: A Pilot Study. (cdc.gov)
Ionotropic glutamat1
In an attempt to discover more potent ligands, we present here a docking study for ionotropic glutamate receptor subtype 6 which is important in many neurodegenerative diseases. (derpharmachemica.com)
Extracellular3
Functions of glutamate transporters include regulation of excitatory neurotransmission , maintenance of low ambient extracellular glutamate concentrations (protects against neurotoxicity) and providing glutamate for metabolism through the glutamate-glutamine cycle. (tocris.com)
Glutamate transporters are essential players in glutamatergic neurotransmission in the brain, where they maintain extracellular glutamate below cytotoxic levels and allow for rounds of transmission. (elifesciences.org)
In this condition, elevated extracellular glutamate causes neuronal loss in many retinal disorders, including glaucoma, ischemia, diabetic retinopathy, and inherited photoreceptor degeneration. (molvis.org)
Excitatory4
Glutamate is the major excitatory neurotransmitter in the CNS, including the cortex and the suprachiasmatic nucleus (SCN). (jneurosci.org)
Excitatory synapses in the brain, which use glutamate as the primary neurotransmitter, represent a crucial target for the action of stress and its mediators. (nature.com)
Glutamate transporters , also known as excitatory amino acid transporters (EAATs), are sodium- and potassium-dependent members of the solute carrier family 6 (SLC1), widely distributed throughout the brain. (tocris.com)
In general, Gi-coupled mGlu receptor subtypes appear to negatively modulate excitatory (and possibly also inhibitory) neurotransmitter output when activated. (aspetjournals.org)
MGluRs2
Conclusion mGluR4 is the main subtype of group Ⅲ mGluRs involved in the regulation of neuropathic pain. (shsmu.edu.cn)
To establish the precise localization of presynaptic mGluRs in the rat hippocampus, we used subtype-specific antibodies for eight mGluRs (mGluR1-mGluR8) for immunohistochemistry combined with lesioning of the three major hippocampal pathways: the perforant path, mossy fiber, and Schaffer collateral. (elsevierpure.com)
GABA2
When you think about glutamate, GABA, and psychedelics, I know you're a clinician, not as much of a researcher as I tend to be sometimes, but what do you think of when you hear, glutamate, GABA, and psychedelics? (psychiatrictimes.com)
Specifically, when I think about glutamate and GABA, I think about the balance between these 2 systems. (psychiatrictimes.com)
Neurotransmitter3
Perturbed homeostasis of the neurotransmitter glutamate is associated with astrocytoma tumor onset and progression, but the factors that govern this phenomenon are less known. (mdpi.com)
Sodium and aspartate symporter Glt Ph is an archaeal homolog of human glutamate transporters, which clear the neurotransmitter glutamate from the synaptic cleft following rounds of neurotransmission ( Danbolt, 2001 ). (elifesciences.org)
Other mGlu subtypes, in particular mGlu2, mGlu8, and possibly mGlu4, are also localized presynaptically, but at perisynaptic sites outside the active zone of neurotransmitter release. (aspetjournals.org)
Selective1
Second, it is highly selective for receptor subtypes. (ub.edu)
Molecular2
We analyzed the molecular mechanisms leading to glutamate release from rat primary cultures of RPE cells, under isosmotic conditions. (molvis.org)
Molecular analysis showed that multiple mammalian-specific mutations have become fixed in the subtype H9N2 viruses, including changes in the hemagglutinin, matrix, and polymerase proteins. (cdc.gov)
Astrocytes3
Suprachiasmatic nucleus (SCN) and cortical astrocytes showed striking differences in sensitivity to glutamate and to mGluR agonists, even after several weeks in culture. (jneurosci.org)
This review discusses the similarities and differences between the morphology of astrocytes and astrocytoma cells, and the role that dysregulation in glutamate and calcium signaling plays in the aberrant morphology of astrocytoma cells. (mdpi.com)
Finally, the cross-talk between glutamate and microglia/astrocytes could involve a positive feedback loop that accelerates excitotoxicity. (springer.com)
Transporters2
Overactivity of glutamate transporters has been implicated in the pathophysiology of schizophrenia and other mental illnesses, whilst underactivity is seen in ischemia and traumatic brain injury. (tocris.com)
Tocris offers the following scientific literature for Glutamate (EAAT) Transporters to showcase our products. (tocris.com)
Neurons2
Modulation of glutamate transmission has been studied extensively in neurons in the CNS. (jneurosci.org)
Given the intimate contact of the RPE with the photoreceptor outer segments, diffusion of RPE-released glutamate could contribute to the excitotoxic death of retinal neurons, and the development of thrombin-induced eye pathologies. (molvis.org)
Metabolism2
Mounting evidence suggests that stress, along with the associated hormonal and neurochemical mediators (particularly glucocorticoids), induces changes in glutamate release, transmission and metabolism in cortical and limbic brain areas, thereby influencing cognitive and emotional processing and behaviour. (nature.com)
Mounting evidence suggests that acute and chronic stress, especially the stress-induced release of glucocorticoids, induces changes in glutamate neurotransmission in the prefrontal cortex and the hippocampus, thereby influencing some aspects of cognitive processing. (nature.com)
19941
Arriza et al (1994) Functional comparisons of three glutamate transporter subtypes cloned from human motor cortex. (tocris.com)
Induces1
Figure 3: Stress induces changes in glutamate receptor trafficking and function in the prefrontal cortex. (nature.com)
Potent1
Potent competitive inhibitor of L-glutamate uptake. (tocris.com)
Mechanisms2
Straightforward pharmacological intervention on different regulatory sites of the glutamate synapse is a possible strategy for bypassing the unmet therapeutic needs posed by traditional drugs based on monoaminergic mechanisms. (nature.com)
Herein, we review possible mechanisms by which glutamate may act in facilitating the growth of projections in astrocytic cells. (mdpi.com)
Voltage-gated1
Ca(2+)-induced Ca2+ release and further influx of Ca2+ through voltage-gated Ca2+ channels after glutamate-induced depolarization contribute to glutamate toxicity. (nih.gov)
Gene2
the remaining gene segments were from the subtype H9N2 G1 clade. (cdc.gov)
Phylogenetic analyses of subtype H9N2 viruses isolated in China and the Middle East have shown that these viruses have undergone reassortment with other subtypes to generate multiple novel genotypes consisting of gene segments from different lineages ( 7 , 11 , 13 , 19 , 20 ). (cdc.gov)
Synapse1
Figure 1: The tripartite glutamate synapse. (nature.com)
Calcium1
We studied modulation of glutamate-evoked calcium rises in primary astrocyte cultures using fura-2 ratiometric digital calcium imaging. (jneurosci.org)
Depression1
There is some thought that low glutamate activity contributes to depression. (dr-bob.org)
Excessive1
The cause of blepharospasm is thought to involve overstimulation of the blink reflex resulting from excessive glutamate stimulation. (addexpharma.com)
Release4
Figure 2: Acute stress rapidly enhances glutamate release in prefrontal and frontal cortex. (nature.com)
These studies along with other evidence suggest that mGlu7 is the nerve terminal autoreceptor that regulates physiological release of glutamate. (aspetjournals.org)
however, the effect of thrombin on glutamate release from RPE cells has not been examined. (molvis.org)
This study showed for the first time that thrombin promotes specific, dose-dependent glutamate release from RPE cells, induced by the activation of protease-activated receptor 1 (PAR-1). (molvis.org)
Specific2
There are five EAAT subtypes, each with a specific distribution. (tocris.com)
The subsequent chapters investigate specific glutamate receptor subtypes. (uu.nl)