A non-essential amino acid. It is found primarily in gelatin and silk fibroin and used therapeutically as a nutrient. It is also a fast inhibitory neurotransmitter.
A family of sodium chloride-dependent neurotransmitter symporters that transport the amino acid GLYCINE. They differ from GLYCINE RECEPTORS, which signal cellular responses to GLYCINE. They are located primarily on the PLASMA MEMBRANE of NEURONS; GLIAL CELLS; EPITHELIAL CELLS; and RED BLOOD CELLS where they remove inhibitory neurotransmitter glycine from the EXTRACELLULAR SPACE.
A class of ionotropic glutamate receptors characterized by affinity for N-methyl-D-aspartate. NMDA receptors have an allosteric binding site for glycine which must be occupied for the channel to open efficiently and a site within the channel itself to which magnesium ions bind in a voltage-dependent manner. The positive voltage dependence of channel conductance and the high permeability of the conducting channel to calcium ions (as well as to monovalent cations) are important in excitotoxicity and neuronal plasticity.
An amino acid intermediate in the metabolism of choline.
Amino acid transporter systems capable of transporting neutral amino acids (AMINO ACIDS, NEUTRAL).
An amino acid that, as the D-isomer, is the defining agonist for the NMDA receptor subtype of glutamate receptors (RECEPTORS, NMDA).
A broad-spectrum excitatory amino acid antagonist used as a research tool.
A worm-like blind tube extension from the CECUM.
Derivatives of GLUTAMIC ACID. Included under this heading are a broad variety of acid forms, salts, esters, and amides that contain the 2-aminopentanedioic acid structure.
Guanosine cyclic 3',5'-(hydrogen phosphate). A guanine nucleotide containing one phosphate group which is esterified to the sugar moiety in both the 3'- and 5'-positions. It is a cellular regulatory agent and has been described as a second messenger. Its levels increase in response to a variety of hormones, including acetylcholine, insulin, and oxytocin and it has been found to activate specific protein kinases. (From Merck Index, 11th ed)
A superorder in the class CEPHALOPODA, consisting of the orders Octopoda (octopus) with over 200 species and Vampyromorpha with a single species. The latter is a phylogenetic relic but holds the key to the origins of Octopoda.
A potent noncompetitive antagonist of the NMDA receptor (RECEPTORS, N-METHYL-D-ASPARTATE) used mainly as a research tool. The drug has been considered for the wide variety of neurodegenerative conditions or disorders in which NMDA receptors may play an important role. Its use has been primarily limited to animal and tissue experiments because of its psychotropic effects.
A superorder of CEPHALOPODS comprised of squid, cuttlefish, and their relatives. Their distinguishing feature is the modification of their fourth pair of arms into tentacles, resulting in 10 limbs.
Cell-surface proteins that bind glutamate and trigger changes which influence the behavior of cells. Glutamate receptors include ionotropic receptors (AMPA, kainate, and N-methyl-D-aspartate receptors), which directly control ion channels, and metabotropic receptors which act through second messenger systems. Glutamate receptors are the most common mediators of fast excitatory synaptic transmission in the central nervous system. They have also been implicated in the mechanisms of memory and of many diseases.
Neuroglial cells of the peripheral nervous system which form the insulating myelin sheaths of peripheral axons.
A class of ionotropic glutamate receptors characterized by their affinity for the agonist AMPA (alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid).
Peptides released by NEURONS as intercellular messengers. Many neuropeptides are also hormones released by non-neuronal cells.
Nerve fibers that are capable of rapidly conducting impulses away from the neuron cell body.

Modulation of long-term synaptic depression in visual cortex by acetylcholine and norepinephrine. (1/6275)

In a slice preparation of rat visual cortex, we discovered that paired-pulse stimulation (PPS) elicits a form of homosynaptic long-term depression (LTD) in the superficial layers when carbachol (CCh) or norepinephrine (NE) is applied concurrently. PPS by itself, or CCh and NE in the absence of synaptic stimulation, produced no lasting change. The LTD induced by PPS in the presence of NE or CCh is of comparable magnitude with that obtained with prolonged low-frequency stimulation (LFS) but requires far fewer stimulation pulses (40 vs 900). The cholinergic facilitation of LTD was blocked by atropine and pirenzepine, suggesting involvement of M1 receptors. The noradrenergic facilitation of LTD was blocked by urapidil and was mimicked by methoxamine, suggesting involvement of alpha1 receptors. beta receptor agonists and antagonists were without effect. Induction of LTD by PPS was inhibited by NMDA receptor blockers (completely in the case of NE; partially in the case of CCh), suggesting that one action of the modulators is to control the gain of NMDA receptor-dependent homosynaptic LTD in visual cortex. We propose that this is a mechanism by which cholinergic and noradrenergic inputs to the neocortex modulate naturally occurring receptive field plasticity.  (+info)

Plasticity of first-order sensory synapses: interactions between homosynaptic long-term potentiation and heterosynaptically evoked dopaminergic potentiation. (2/6275)

Persistent potentiations of the chemical and electrotonic components of the eighth nerve (NVIII) EPSP recorded in vivo in the goldfish reticulospinal neuron, the Mauthner cell, can be evoked by afferent tetanization or local dendritic application of an endogenous transmitter, dopamine (3-hydroxytyramine). These modifications are attributable to the activation of distinct intracellular kinase cascades. Although dopamine-evoked potentiation (DEP) is mediated by the cAMP-dependent protein kinase (PKA), tetanization most likely activates a Ca2+-dependent protein kinase via an increased intracellular Ca2+ concentration. We present evidence that the eighth nerve tetanus that induces LTP does not act by triggering dopamine release, because it is evoked in the presence of a broad spectrum of dopamine antagonists. To test for interactions between these pathways, we applied the potentiating paradigms sequentially. When dopamine was applied first, tetanization produced additional potentiation of the mixed synaptic response, but when the sequence was reversed, DEP was occluded, indicating that the synapses potentiated by the two procedures belong to the same or overlapping populations. Experiments were conducted to determine interactions between the underlying regulatory mechanisms and the level of their convergence. Inhibiting PKA does not impede tetanus-induced LTP, and chelating postsynaptic Ca2+ with BAPTA does not block DEP, indicating that the initial steps of the induction processes are independent. Pharmacological and voltage-clamp analyses indicate that the two pathways converge on functional AMPA/kainate receptors for the chemically mediated EPSP and gap junctions for the electrotonic component or at intermediaries common to both pathways. A cellular model incorporating these interactions is proposed on the basis of differential modulation of synaptic responses via receptor-protein phosphorylation.  (+info)

Low resting potential and postnatal upregulation of NMDA receptors may cause Cajal-Retzius cell death. (3/6275)

Using in situ patch-clamp techniques in rat telencephalic slices, we have followed resting potential (RP) properties and the functional expression of NMDA receptors in neocortical Cajal-Retzius (CR) cells from embryonic day 18 to postnatal day 13, the time around which these cells normally disappear. We find that throughout their lives CR cells have a relatively depolarized RP (approximately -50 mV), which can be made more hyperpolarized (approximately -70 mV) by stimulation of the Na/K pump with intracellular ATP. The NMDA receptors of CR cells are subjected to intense postnatal upregulation, but their similar properties (EC50, Hill number, sensitivity to antagonists, conductance, and kinetics) throughout development suggest that their subunit composition remains relatively homogeneous. The low RP of CR cells is within a range that allows for the relief of NMDA channels from Mg2+ blockade. Our findings are consistent with the hypothesis that CR cells may degenerate and die subsequent to uncontrolled overload of intracellular Ca2+ via NMDA receptor activation by ambient glutamate. In support of this hypothesis we have obtained evidence showing the protection of CR cells via in vivo blockade of NMDA receptors with dizocilpine.  (+info)

Ischemic tolerance in murine cortical cell culture: critical role for NMDA receptors. (4/6275)

Murine cortical cultures containing both neurons and glia (days in vitro 13-15) were exposed to periods of oxygen-glucose deprivation (5-30 min) too brief to induce neuronal death. Cultures "preconditioned" by sublethal oxygen-glucose deprivation exhibited 30-50% less neuronal death than controls when exposed to a 45-55 min period of oxygen-glucose deprivation 24 hr later. This preconditioning-induced neuroprotection was specific in that neuronal death induced by exposure to excitotoxins or to staurosporine was not attenuated. Neuroprotection was lost if the time between the preconditioning and severe insult were decreased to 7 hr or increased to 72 hr and was blocked if the NMDA antagonist 100 microM 3-((D)-2-carboxypiperazin-4-yl)-propyl-1-phosphonic acid was applied during the preconditioning insult. This was true even if the duration of preconditioning was increased as far as possible (while still remaining sublethal). A similar preconditioning effect was also produced by sublethal exposure to high K+, glutamate, or NMDA but not to kainate or trans-1-aminocyclopentane-1, 3-dicarboxylic acid.  (+info)

Single synaptic events evoke NMDA receptor-mediated release of calcium from internal stores in hippocampal dendritic spines. (5/6275)

We have used confocal microscopy to monitor synaptically evoked Ca2+ transients in the dendritic spines of hippocampal pyramidal cells. Individual spines respond to single afferent stimuli (<0.1 Hz) with Ca2+ transients or failures, reflecting the probability of transmitter release at the activated synapse. Both AMPA and NMDA glutamate receptor antagonists block the synaptically evoked Ca2+ transients; the block by AMPA antagonists is relieved by low Mg2+. The Ca2+ transients are mainly due to the release of calcium from internal stores, since they are abolished by antagonists of calcium-induced calcium release (CICR); CICR antagonists, however, do not depress spine Ca2+ transients generated by backpropagating action potentials. These results have implications for synaptic plasticity, since they show that synaptic stimulation can activate NMDA receptors, evoking substantial Ca2+ release from the internal stores in spines without inducing long-term potentiation (LTP) or depression (LTD).  (+info)

Changes in protein tyrosine phosphorylation in the rat brain after cerebral ischemia in a model of ischemic tolerance. (6/6275)

A brief period of sublethal cerebral ischemia, followed by several days of recovery, renders the brain resistant to a subsequent lethal ischemic insult, a phenomenon termed ischemic preconditioning or tolerance. Ischemic tolerance was established in the rat two-vessel occlusion model of ischemia, induced by occlusion of both carotid arteries in combination with hypotension. Ischemic preconditioning (3 minutes) provided maximal neuroprotection when induced 2 days prior to a lethal ischemic insult of 9-minute duration. Neuroprotection persisted for at least 8 weeks. Since neurotransmission has been implicated in ischemic cell death, the effect of ischemic preconditioning on tyrosine phosphorylation of proteins and on the levels of glutamate receptor subunits in hippocampus and neocortex was studied. Regional levels of tyrosine phosphorylation of proteins in general and the N-methyl-D-aspartate receptor subunit NR2 in particular are markedly enhanced after ischemia in nonconditioned brains, in both the synaptosomal fraction and the whole-tissue homogenate of rat neocortex and hippocampus, but recover to control levels only in the preconditioned brain. Ischemic preconditioning selectively induces a decrease in the levels of the NR2A and NR2B subunits and a modest decrease in the levels of NR1 subunit proteins in the synaptosomal fraction of the neocortex but not hippocampus after the second lethal ischemia. It was concluded that ischemic preconditioning prevents a persistent change in cell signaling as evidenced by the tyrosine phosphorylation of proteins after the second lethal ischemic insult, which may abrogate the activation of detrimental cellular processes leading to cell death.  (+info)

Impairment of neocortical long-term potentiation in mice deficient of endothelial nitric oxide synthase. (7/6275)

The role of the possible retrograde messenger nitric oxide (NO) in the induction of long-term potentiation (LTP) was studied in supragranular layers of somatosensory cortical slices obtained from adult mice. High-frequency stimulation produced a slowly rising, long-lasting (50 min) and significant (P < 0.001) increase in the extracellular synaptic response by 23%. The induction of LTP was independent from activation of N-methyl-D-aspartate (NMDA) receptors, but prevented by bath application of NG-nitro-L-arginine methyl ester (L-NAME), indicating that one or several of the different NO synthases (NOS) produced NO within the postsynaptic neuron. No LTP could be induced in knockout mice lacking the endothelial NOS (eNOS) isoform. These data suggest that eNOS is involved in an NMDA receptor-independent form of LTP in the rodent cerebral cortex.  (+info)

17beta-estradiol enhances NMDA receptor-mediated EPSPs and long-term potentiation. (8/6275)

Gonadal steroid hormones influence CNS functioning through a variety of different mechanisms. To test the hypothesis that estrogen modulates synaptic plasticity in the hippocampus, in vitro hippocampal slices from 2-mo-old Sprague-Dawley male rats were used to determine the effect of 17beta-estradiol on both N-methyl-D-aspartate (NMDA) receptor-mediated excitatory postsynaptic potentials (EPSPs) through intracellular recordings and long-term potentiation (LTP) through extracellular recordings. Intracellular EPSPs and extracellular field EPSPs (fEPSPs) were recorded from CA1 pyramidal cells by stimulating Schaffer collateral fibers. In intracellular experiments, slices were perfused with medium containing bicuculline (5 microM) and low Mg2+ (0.1 mM) to enhance the NMDA receptor-mediated currents and 6, 7-dinitroquinoxaline-2,3-dione (DNQX) (10 microM) to block the alpha-amino-3-hydroxy-5-methyl-4-isoxazoleproprianate (AMPA) receptor-mediated component. The effects of 17beta-estradiol on NMDA receptor-mediated activity were excitatory; concentrations >10 nM induced seizure activity, and lower concentrations (1 nM) markedly increased the amplitude of NMDA-mediated EPSPs (both the first and second responses increased during paired pulse stimulation by 180 and 197%, respectively). In extracellular experiments, slices perfused with 17beta-estradiol (100 pM) exhibited a pronounced, persisting, and significant enhancement of LTP of both the fEPSP slope (192%) and fEPSP amplitude (177%) compared with control slices (fEPSP slope = 155%; fEPSP amplitude = 156%) 30 min after high-frequency stimulation. These data demonstrate that estrogen enhances NMDA receptor-mediated currents and promotes an enhancement of LTP magnitude.  (+info)

Physiological activation of the N-methyl-D-aspartate (NMDA) subtype of glutamate receptors has been proposed to play a key role in both neuronal cell function and dysfunction. In the present study, we used selective NMDA receptor antagonists to investigate the involvement of NR2A and NR2B subunits in the modulatory effect of basal NMDA receptor activity on the phosphorylation of Tau proteins. We observed, in acute hippocampal slice preparations, that blockade of NR2A-containing NMDA receptors by the NR2A antagonist NVP-AAM077 provoked the hyperphosphorylation of a residue located in the proline-rich domain of Tau (i.e., Ser199). This effect seemed to be Ser199 specific as there was no increase in phosphorylation at Ser262 and Ser409 residues located in the microtubule-binding and C-terminal domains of Tau proteins, respectively. From a mechanistic perspective, our study revealed that blockade of NR2A-containing receptors influences Tau phosphorylation probably by increasing calcium influx into neurons,
Expressions of N-methyl-D-aspartate receptors NR2A and NR2B subunit proteins in normal and sulfite-oxidase deficient rats hippocampus: effect of exogenous sulf
Pharmacological, genetic and expression studies implicate N-methyl-D-aspartate (NMDA) receptor hypofunction in schizophrenia (SCZ). Similarly, several lines of evidence suggest that autism spectrum disorders (ASD) could be due to an imbalance between excitatory and inhibitory neurotransmission. As part of a project aimed at exploring rare and/or de novo mutations in neurodevelopmental disorders, we have sequenced the seven genes encoding for NMDA receptor subunits (NMDARs) in a large cohort of individuals affected with SCZ or ASD (n=429 and 428, respectively), parents of these subjects and controls (n=568). Here, we identified two de novo mutations in patients with sporadic SCZ in GRIN2A and one de novo mutation in GRIN2B in a patient with ASD. Truncating mutations in GRIN2C, GRIN3A and GRIN3B were identified in both subjects and controls, but no truncating mutations were found in the GRIN1, GRIN2A, GRIN2B and GRIN2D genes, both in patients and controls, suggesting that these subunits are critical for
To identify the protein kinases regulating synaptic NMDA receptors, as well as the conditions favoring enhancement of NMDA receptor-mediated excitatory postsynaptic currents (EPSCs) by phosphorylation, we studied the effects of kinase activation and inhibition in hippocampal neurons. Inhibition of c …
TY - JOUR. T1 - Pharmacology of ACEA-1416. T2 - A potent systemically active NMDA receptor glycine site antagonist. AU - Ilyin, Victor I.. AU - Whittemore, Edward R.. AU - Tran, Minhtam. AU - Shen, Ke-Zhong. AU - Cai, Sui Xiong. AU - Kher, Sunil M.. AU - Keana, John F W. AU - Weber, Eckard. AU - Woodward, Richard M.. PY - 1996/8/29. Y1 - 1996/8/29. N2 - Excitatory amino acid receptor antagonists show potential for the treatment of ischemic stroke and head trauma. In search of novel antagonists, a series of alkyl- and alkoxyl-substituted 1,4-dihydro-2,3-quinoxalinediones were synthesized and assayed for inhibition of glutamate receptors. We report on the pharmacological characterization of one such compound, 7-chloro-6-methyl-5-nitro-1,4-dihydro-2,3-quinoxalinedione (ACEA-1416). Electrophysiological assays showed that ACEA-1416 is a potent antagonist of rat brain NMDA receptors expressed in Xenopus oocytes, and NMDA receptors expressed by cultured rat cortical neurons. Antagonism is via ...
Long-term potentiation of NMDA-receptor-mediated synaptic transmission (NMDAR-LTP) is a little-understood form of plasticity. In the present study, we investigated whether NMDAR-LTP in the dentate gyrus involves recruitment of extrasynaptic NMDARs, because NMDARs are expressed both synaptically and extrasynaptically with evidence for subtype differences at different locations. We show that before induction of NMDAR-LTP, pharmacological inhibition of glutamate transporters resulted in glutamate spillover from the synapse and activation of extrasynaptic NMDARs. After the induction of NMDAR-LTP, such activation of extrasynaptic NMDARs was absent. Activation of extrasynaptic NMDARs after glutamate uptake inhibition also occurred when synaptic NMDARs were inhibited with MK801 [(+)-5-methyl-10,11-dihydro-5H-dibenzo [a,d] cyclohepten-5,10-imine maleate], and this extrasynaptically mediated NMDAR-EPSC was strongly reduced by prior induction of NMDAR-LTP. The extrasynaptic NMDARs were shown to be ...
2In slices, the potencies of the weakly (or non-) transported analogues, N-methyl-D-aspartate (NMDA) and kainate (KA) (EC50 = 40 μM each) were higher than those of the transported amino acids, D- and L-aspartate (EC50 = 250 μM and 300 μM) and D- and L-glutamate (EC50 = 540 μM and 480 μM). Quisqualate (up to 300 μM) failed to increase cyclic GMP levels significantly. The sensitivity of agonist responses to the NMDA receptor antagonist, DL-2-amino-5-phosphonovalerate (APV), was in the order NMDA , L-aspartate , L-glutamate, KA ...
N-Methyl-d-aspartate receptors (NMDAR) are involved in the regulation of alcohol drinking, but the contribution of NMDAR subunits located on specific neuronal populations remains incompletely understood. The current study examined the role of GluN2B-containing NMDARs expressed on cortical principal neurons and cortical interneurons in mouse ethanol drinking. Consumption of escalating concentrations of ethanol was measured in mice with GluN2B gene deletion in either cortical principal neurons (GluN2B(CxNULL)) or interneurons (GluN2B(InterNULL)), using a two-bottle choice paradigm. Results showed that GluN2B(InterNULL), but not GluN2B(CxNULL), mice consumed significantly less ethanol, at relatively high concentrations, than non-mutant controls. In a second paradigm in which mice were offered a 15% ethanol concentration, without escalation, GluN2B(CxNULL) mice were again no different from controls. These findings provide novel evidence for a contribution of interneuronal GluN2B-containing NMDARs in ...
Toxicol Lett. 2011 Sep 10;205(3):336-40. Epub 2011 Jun 24. Chen HH, Lin YR, Chan MH. Source Institute of Pharmacology and Toxicology, Tzu Chi University, 701, Sec. 3, Chung Yang Rd., Hualien 97004, Taiwan. Abstract Toluene, an industrial organic solvent, is voluntarily inhaled as drug of abuse. Because inhibition of N-methyl-d-aspartate (NMDA) receptors is one of…
Background Proof from both animal and human studies clearly supports the renal beneficial effects of empagliflozin (emp), a sodium glucose co-transporter 2 (SGLT2) inhibitor, but the mechanism in which it exerts its effect is not well understood. increased expression of Collagen IV, Fibronectin, transforming growth factor-beta1 (TGF-1). However, emp treatment remarkably decreased expression of TGF-1, accumulation of extracellular matrix proteins (Fibronectin, Collagen IV), as well as (phosphorylated-smad3) P-smad3. HG increased SGLT2 protein expression compared to normal glucose (NG) Bivalirudin Trifluoroacetate while emp significantly decreased SGLT2 expression. Furthermore, emp decreased high glucose-induced alpha-smooth muscle actin (-SMA) expression and reversed epithelial marker (E-catherin) suppression induced by high glucose. In addition, emp treatment for 72 h increased expression of HIF-1 protein (95% CI: -0.5918 to C0.002338, at 100nM, P 0.05, 95% CI C0.6631 to C0.07367 at 500nM, P ...
The activation of the N-methyl-D-aspartate receptor (NMDAR) is critical for the induction of synaptic plasticity in the hippocampus. Aging can alter glutamatergic synaptic transmission in the hippocampus, and cognitive impairments in aged animals are accompanied by reduced NMDARmediated plasticity at Schaffer collateral-CA1 synapses. However, the specific contribution of NMDAR subunits to NMDAR-mediated synaptic responses in aged tissue has not yet been fully understood. The main purpose of present study was to examine whether there is an impact of aging on NMDAR subunit expression and whether synaptic plasticity may depend on NMDAR subunit composition in the aged hippocampus ...
In this study, N-methyl-D-aspartate (NMDA)-receptor antagonists enhanced the head-twitch response induced by 5-hydroxytryptamine (5-HT) in reserpine-treated mice. To minimize the risk of any indirect involvement of NMDA-receptor antagonists (D(-)-2-amino-5-phosphonopentanoic acid (AP-5), D(-)-3-(2-carboxypiperazine-4-yl)-propyl-1-phosphonic acid (CPP), (+)-5-methyl-10,11-dihydroxy-5H-dibenzo-[a,d]-cyclohepten-5,10-imi ne (MK-801), ketamine, dextrorphan and dextromethorphan) with 5-HT neurones, vesicle stores of monoamines, especially 5-HT, were depleted with reserpine. In addition, the enhancement of 5-HT-induced head-twitch response was inhibited by apomorphine and NMDA as well as ritanserin in reserpine-treated mice. These results support our previous conclusion that NMDA receptors play important roles in the glutamatergic modulation of 5-HTergic function at the postsynaptic 5-HT2 receptors in mice ...
Characterization of the cerebroprotective efficacy of the competitive NMDA receptor antagonist CGP40116 in a rat model of focal cerebral ischemia: an in vivo magnetic resonance imaging study. - D Sauer, P R Allegrini, A Cosenti, A Pataki, H Amacker, G E Fagg
Long-term learning and memory require long-lasting changes in the strength of specific synaptic connections between neurons (Martin et al., 2000; Kandel, 2001). These adaptive changes in synaptic efficacy are initiated by activity-dependent release of neurotransmitters from presynaptic nerve terminals and binding to their cognate postsynaptic receptors. In glutamatergic synapses of the hippocampus, many of the activity-dependent synaptic modifications require the participation of NMDA receptors, which are heteromultimeric ion channels composed of the NR1 subunit and one or more of the NR2A or NR2B subunits (Hollmann and Heinemann, 1994). NMDA receptor-dependent Ca2+ influx activates a cascade of biochemical events that lead to the activation of so-called immediate early genes (IEGs). IEGs regulate delayed onset of effector genes, coding for structural, growth-related, and synaptic proteins (Herdegen and Leah, 1998). A candidate molecule suggested to participate in learning and memory is the IEG ...
In the present study, N-methyl-D-aspartate receptor 2B (NR2B)-specific siRNA was applied in parkinsonian models. Our previous results showed that reduction in expression of N-methyl-D-aspartate receptor 1 (NR1), the key subunit of N-methyl-D-aspartate receptors, by antisense oligos ameliorated the motor symptoms in the 6-hydroxydopamine (6-OHDA)-lesioned rat, an animal model of Parkinsons disease (PD) [Lai et al.: Neurochem Int 2004;45:11-22]. To further the investigation on the efficacy of gene silencing, small interference RNA (siRNA) specific for the NR2B subunit was designed and administered in the striatum of 6-OHDA-lesioned rats. The present results show that administration of NR2B-specific siRNA decreased the number of apomorphine-induced rotations in the lesioned rats and that there was a significant reduction in NR2B proteins levels after NR2B-specific siRNA administration. Furthermore, attenuation of the loss of dopaminergic neurons was found in both the striatal and substantia nigra ...
Long-term potentiation (LTP) in the hippocampal CA1 region requires the activation of N-methyl-D-aspartate receptors (NMDARs). Studies using genetic and pharmacological approaches have reported inconsistent results of the requirement of NR2B-containing NMDARs in LTP in the CA1 region. Pharmacological studies showed that NR2B-containing NMDARs are not required for LTP, while genetic studies reported that over-expression of NR2B-NMDARs enhances LTP and hippocampus-dependent memory. Here, we provide evidence showing that the functional role of NR2B-NMDARs in hippocampal LTP and memory depends on LTP-inducing and behavior-conditioning protocols. Inhibition of NR2B-NMDARs with the NR2B selective antagonist ifenprodil or Ro25-6981 suppressed LTP induced by spike-timing protocol, with no impact on LTP induced by pairing protocol or two-train high-frequency stimulation (HFS) protocol. Inhibition of NR2B-NMDARs did not affect the late phase LTP induced by four-train HFS. Ca2+ imaging showed that there was
The N-methyl-d-aspartate receptor plays a critical role in the formation and maintenance of synapses during brain development. In the rodent, changes in subunit expression and assembly of the heteromeric receptor complex accompany these maturational processes. However, little is known about N-methyl-d-aspartate receptor subunit expression during human brain development. We used in situ hybridization to examine the distribution and relative abundance of NR1, NR2A and NR2B subunit messenger ribonucleic acids in the hippocampal formation and adjacent cortex of 34 human subjects at five stages of life (neonate, infant, adolescent, young adult and adult). At all ages, the three messenger ribonucleic acids were expressed in all subfields, predominantly by pyramidal neurons, granule cells and polymorphic hilar cells. However, their abundance varied across ontogeny. Levels of NR1 messenger ribonucleic acid in CA4, CA3 and CA2 subfields were significantly lower in the neonate than all other age groups. In the
The N-methyl-d-aspartate receptor plays a critical role in the formation and maintenance of synapses during brain development. In the rodent, changes in subunit expression and assembly of the heteromeric receptor complex accompany these maturational processes. However, little is known about N-methyl-d-aspartate receptor subunit expression during human brain development. We used in situ hybridization to examine the distribution and relative abundance of NR1, NR2A and NR2B subunit messenger ribonucleic acids in the hippocampal formation and adjacent cortex of 34 human subjects at five stages of life (neonate, infant, adolescent, young adult and adult). At all ages, the three messenger ribonucleic acids were expressed in all subfields, predominantly by pyramidal neurons, granule cells and polymorphic hilar cells. However, their abundance varied across ontogeny. Levels of NR1 messenger ribonucleic acid in CA4, CA3 and CA2 subfields were significantly lower in the neonate than all other age groups. In the
TY - JOUR. T1 - Phosphatidylinositol 3-kinase is a central mediator of NMDA receptor signalling to MAP kinase (Erk1/2), Akt/PKB and CREB in striatal neurones. AU - Perkinton, Michael S. AU - Ip, James K. AU - Wood, Gemma L. AU - Crossthwaite, Andrew J. AU - Williams, Robert J. PY - 2002. Y1 - 2002. N2 - Ca2+ influx through NMDA receptors can initiate molecular changes in neurones which may underlie synaptic plasticity, neuronal development, survival and excitotoxicity. Signalling through the MAP kinase (Erk1/2) cascade may be central to these processes. We previously demonstrated that Ca2+-permeable AMPA receptors activate Erkl/2 through a phosphatidylinositol 3-kinase (PI 3-kinase)-dependent mechanism. We now report that NMDA receptor activation of Erk1/2 was also blocked by inhibitors of PI 3-kinase (LY 294002, wortmannin). In addition, pre-treatment of neurones with pertussis toxin inhibited NMDA-induced Erk1/2 activation, indicating a role for heterotrimeric Gi/o proteins. PI 3-kinase ...
This study shows that NMDA receptor-driven plasticity, behavior, and signal transduction is mediated by the MAGUK protein SAP102. SAP102 was required for the induction or initiation of these signaling events consistent with its direct physical association with the receptor. Remarkable specificity in the signaling responses was observed, with only specific frequencies of synaptic activation requiring SAP102 and ERK pathways. Thus, the discrimination of different patterns of neuronal activity, all of which activate the NMDA receptor, is performed by distinct MAGUK proteins that then selectively engage downstream pathways. These results are consistent with published experiments showing MAGUK selectivity in relation to NMDA receptor subunits, downstream signaling, and plasticity effector mechanisms. Biochemical and electrophysiological evidence suggests that PSD-95 preferentially associates with NR2A-containing NMDA receptors, whereas SAP102 associates with NR2B-containing receptors (Sans et al., ...
GluN2B/NR2b glutamate receptor, also known as Glutamate/N-methyl D-aspartate/NMDA receptor subtype 2B, is a member of the NMDA receptor family. NMDA receptors are expressed throughout the CNS in postsynaptic cell membranes. GluN2B is a major NMDAR subtype found in cortical and hippocampal regions of the adult brain. NMDA receptors are involved with memory and learning. Mutations in the gene encoding GluN2B are associated with autism, LennoxGastaut and West Syndromes ...
QNZ46 is a NMDA receptor antagonist. QNZ46 inhibits NMDA receptor function in a noncompetitive and voltage-independent manner by an unconventional mechanism that requires binding of glutamate to the GluN2 subunit, but not glycine binding to the GluN1 subunit. QNZ46 could provide an opportunity for the development of pharmacological tools and therapeutic agents that target NMDA receptors at a new site and modulate function by a novel mechanism. NMDA receptors are ionotropic glutamate receptors that mediate excitatory synaptic transmission and have been implicated in several neurological diseases.
TY - JOUR. T1 - Nerve Growth Factor Uses Ras/ERK and Phosphatidylinositol 3-Kinase Cascades to Up-regulate the N-Methyl-D-aspartate Receptor 1 Promoter. AU - Liu, Anguo. AU - Prenger, Michael S.. AU - Norton, Darrell D.. AU - Mei, Lin. AU - Kusiak, John W.. AU - Bai, Guang. PY - 2001/11/30. Y1 - 2001/11/30. N2 - We reported previously that nerve growth factor (NGF) up-regulates activity of the N-methyl-D-aspartate receptor 1 (NR1) promoter. We have explored the pathways and nuclear targets of NGF signaling in regulating the NR1 promoter. PD98059 and wortmannin, but not rapamycin, significantly attenuated NGF-induced transcriptional activity from an NR1 promoter-luciferase construct. Coexpressing constitutively active forms of Ras, Raf, or MAPK/ERK kinase 1 (MEK1) increased promoter activity dramatically. The MEK1-induced increase was largely prevented by mutations of the tandem GC boxes in the promoter. Promoter activity was also increased significantly by coexpressed GC box-binding proteins ...
Ketamine, an FDA approved anesthetic agent, is becoming the sedative/analgesic of choice for emergency sedation in children because it causes deep sedation with minimal respiratory depression in comparison to other available agents. However, emergence reactions are an important adverse effect of ketamine, characterized by transient changes in cognitive function, dissociation and mild schizophrenia-like symptoms. These cognitive and behavioral effects are dose-dependently induced by ketamine and other antagonists of the N-methyl-D-aspartate (NMDA) glutamate receptor. NMDA receptor hypofunction can disinhibit excitatory (cholinergic/glutamatergic) projections in key areas of the brain, and this has been proposed to explain key features of schizophrenia. Several treatments that block excessive excitatory transmitter release have also been shown to prevent cognitive and behavioral effects of ketamine-induced NMDA receptor hypofunction in humans. Alpha-2 adrenergic agonists, which can presynaptically ...
Ketamine, an FDA approved anesthetic agent, is becoming the sedative/analgesic of choice for emergency sedation in children because it causes deep sedation with minimal respiratory depression in comparison to other available agents. However, emergence reactions are an important adverse effect of ketamine, characterized by transient changes in cognitive function, dissociation and mild schizophrenia-like symptoms. These cognitive and behavioral effects are dose-dependently induced by ketamine and other antagonists of the N-methyl-D-aspartate (NMDA) glutamate receptor. NMDA receptor hypofunction can disinhibit excitatory (cholinergic/glutamatergic) projections in key areas of the brain, and this has been proposed to explain key features of schizophrenia. Several treatments that block excessive excitatory transmitter release have also been shown to prevent cognitive and behavioral effects of ketamine-induced NMDA receptor hypofunction in humans. Alpha-2 adrenergic agonists, which can presynaptically ...
After cerebral ischemia, the loss of blood supply triggers a series of pathological changes known as ischemic cascades. One of the key components of this cascade is excitotoxicity, triggered by the excessive extracellular glutamate level, overactivation of N-methyl-D-aspartate (NMDA)-glutamate subty
NMDA receptors are glutamate- and glycine-gated channels that mediate fast excitatory transmission in the central nervous system and are critical to synaptic development, plasticity and integration. They have a rich complement of modulatory sites, which represent important pharmacologic targets. Ifenprodil is a well-tolerated NMDA receptor inhibitor; it is selective for GluN2B-containing receptors; and has neuroprotective effects. The mechanism by which ifenprodil inhibits NMDA receptor responses is not fully understood. The inhibition is incomplete and non-competitive with other known NMDA receptor agonists or modulators, although reciprocal effects have been reported between ifenprodil potency and that of extracellular ligands including glutamate, glycine, zinc, protons and polyamines. Recently, structural studies revealed that ifenprodil binds to a unique site at the interface between the extracellular N-termini of GluN1 and GluN2B subunits supporting the view that interactions with other ...
N-methyl-d-aspartate receptor (NMDAR) subunit composition strictly commands receptor function and pharmacological responses. Changes in NMDAR subunit composition have been documented in brain disorders such as Parkinsons disease (PD) and levodopa (L-DOPA)-induced dyskinesias (LIDs), where an increase of NMDAR GluN2A/GluN2B subunit ratio at striatal synapses has been observed. A therapeutic approach aimed at rebalancing NMDAR synaptic composition represents a valuable strategy for PD and LIDs. To this, the comprehension of the molecular mechanisms regulating the synaptic localization of different NMDAR subtypes is required. We have recently demonstrated that Rabphilin 3A (Rph3A) is a new binding partner of NMDARs containing the GluN2A subunit and that it plays a crucial function in the synaptic stabilization of these receptors. Considering that protein-protein interactions govern the synaptic retention of NMDARs, the purpose of this work was to analyse the role of Rph3A and Rph3A/NMDAR complex ...
TY - JOUR. T1 - Hypoxia modulates nitric oxide-induced regulation of NMDA receptor currents and neuronal cell death. AU - Gbadegesin, Muyiwa. AU - Vicini, Stefano. AU - Hewett, Sandra. AU - Wink, David A.. AU - Espey, Michael. AU - Pluta, Ryszard M.. AU - Colton, Carol A.. PY - 1999. Y1 - 1999. N2 - Nitric oxide (NO) released from a new chemical class of donors enhances N-methyl-D-aspartate (NMDA) channel activity. Using whole cell and single- channel patch-clamp techniques, we have shown that (Z)-1-[N(3-ammoniopropyl)- N-(n-propyl)amino]-NO (PAPA-NO) and diethylamine NO, commonly termed NONOates, potentiate the glutamate-mediated response of recombinant rat NMDA receptors(NR1/NR2A) expressed in HEK-293 cells. The overall effect is an increase in both peak and steady-state whole cell currents induced by glutamate. Single-channel studies demonstrate a significant increase in open probability but no change in the mean single-channel open time or mean channel conductance. Reduction in oxygen levels ...
We report here that brief exposure to 5-50 μM extracellular zinc, comparable to the concentrations estimated to be released normally into synaptic clefts (4), selectively enhanced the phosphorylation of neuronal Src at tyrosine 220 in the SH2 domain, without affecting tyrosine phosphorylation of Fyn. This phosphorylation was accompanied by increases in Src activity, NMDA receptor phosphorylation, and NMDA receptor function (current and excitotoxicity). Drawing on key earlier studies as well as present measurements of [Na+]i in neurons exposed to zinc, we propose that the ability of zinc to induce this up-regulation of Src activity and NMDA receptor function is mediated by inhibition of plasma membrane Na+/K+ ATPase and elevated [Na+]i. Although low concentrations of zinc can potentiate current mediated by certain homomeric NMDA receptor subunit 1 (NR1) splice variants, zinc potentiation of more physiological heteromeric NR1/NR2 receptors was not previously observed (70, 71).. No change in the ...
TY - JOUR. T1 - Na+ occupancy and Mg2+ block of the N-methyl-D-aspartate receptor channel. AU - Zhu, Yongling. AU - Auerbach, Anthony. PY - 2001. Y1 - 2001. N2 - The effect of extracellular and intracellular Na+ on the single-channel kinetics of Mg2+ block was studied in recombinant NR1-NR2B NMDA receptor channels. Na+ prevents Mg2+ access to its blocking site by occupying two sites in the external portion of the permeation pathway. The occupancy of these sites by intracellular, but not extracellular, Na+ is voltage-dependent. In the absence of competing ions, Mg2+ binds rapidly (,108 M-1s-1, with no membrane potential) to a site that is located 0.60 through the electric field from the extracellular surface. Occupancy of one of the external sites by Na+ may be sufficient to prevent Mg2+ dissociation from the channel back to the extracellular compartment. With no membrane potential; and in the absence of competing ions, the Mg2+ dissociation rate constant is ,10 times greater than the Mg2+ ...
Dr. Graham L. Collingridge accepted the invitation on 18 March 2007 (self-imposed deadline: 18 June 2007). This article will briefly cover: The discovery of the NMDA receptor, its unusual properties (Mg block, slow kinetics, Ca permeability, voltage-dependence, glycine co-agonist site), its role in synaptic transmission, synaptic plasticity and diseases. The NMDA receptor is one of the four major classes of receptors that respond to L-glutamate, the major excitatory neurotransmitter in the brain. It is named after the synthetic chemical N-methyl-D-aspartate, which is a highly selective agonist for this receptor. THe NMDA receptor (NMDAR) has unique properties that distinguishes it from the other three major glutamate receptor classes - AMPA receptors, kainate receptors and metabotropic receptors. The NMDAR is a tetramer, which is made up from various combinations of the subunits NR1, NR2A, NR2B, NR2C, NR2D, NR3A and NR3B. Most NMDARs contain 2 NR1 subunits, which bind the co-agonist glycine and ...
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It has long been accepted that high concentrations of glutamate can destroy neurons, and this is the basis of the theory of excitotoxicity during brain injury such as stroke. Glutamate N-methyl-D-aspartate (NMDA) receptor antagonists such as Selfotel, Aptiganel, Gavestinel and others failed to show neuroprotective efficacy in human clinical trials or produced intolerable central nervous system adverse effects. The failure of these agents has been attributed to poor studies in animal models and to poorly designed clinical trials. We also speculate that NMDA receptor antagonism may have hindered endogenous mechanisms for neuronal survival and neuroregeneration. It remains to be proven in human stroke whether NMDA receptor antagonism can be neuroprotective.
Sigma-Aldrich offers abstracts and full-text articles by [Liana Roberts Stein, Charles F Zorumski, Shin-Ichiro Imai, Yukitoshi Izumi].
TY - JOUR. T1 - Prenatal NMDA receptor antagonism impaired proliferation of neuronal progenitor, leading to fewer glutamatergic neurons in the prefrontal cortex. AU - Toriumi, Kazuya. AU - Mouri, Akihiro. AU - Narusawa, Shiho. AU - Aoyama, Yuki. AU - Ikawa, Natsumi. AU - Lu, Lingling. AU - Nagai, Taku. AU - Mamiya, Takayoshi. AU - Kim, Hyoung Chun. AU - Nabeshima, Toshitaka. N1 - Funding Information: We thank Dr Furukawa H for synthesizing PCP. This study was supported by Grants-in-aid for Scientific Research (A) (22248033), Scientific Research (B) (20390073) (21390045) and Exploratory Research from the JSPS (19659017) (22659213); by the Academic Frontier Project for Private Universities (2007-2011) from the Ministry of Education, Culture, Sports, Science and Technology of Japan (MEXT); by Regional Joint Research Program supported by grants to Private Universities to Cover Current Expenses from MEXT; by Research on Regulatory Science of Pharmaceuticals and Medical Devices from the Ministry of ...
Neuroprotective efficiency of NMDA receptor blockade in the striatum and CA3 hippocampus after various durations of cerebral ischemia in gerbils. - L Radenovic, V Selakovic, B Janac, Pavle R Andjus
In a recent BNN article on potential drugs for memory loss, we omitted two conventional classes of drugs used to treat Alzheimers Disease-acetylcholine esterase inhibitors (AChE-Is) and the blocker of glutamate NMDA receptors memantine (Namenda). This was intentional, as we hoped to suggest possible approaches prior to the use of these drugs for full-blown dementia. However, we neglected to cite a 1999 study by Fred Jacobsen in the Journal of Clinical Psychiatry that indicated that the AChE-I drug donepezil (Aricept) was effective in improving drug-induced memory dysfunction in patients without dementia. Side effects included insomnia, nausea, vomiting, and diarrhea.. Jacobsen has used AChE-Is to improve memory in over 80 patients with unipolar or bipolar depression, aged 19-85. In a 2016 personal communication to the BNN, he indicated that doses of 5mg/day are typically enough to improve memory. Higher doses of 10mg/day may be more effective, but increase the risk of switching into mania for ...
Qin S, Zhao X, Pan Y, Liu J, Feng G, Fu J, Bao J, Zhang Z, He L. An association study of the N-methyl-D-aspartate receptor NR1 subunit gene (GRIN1) and NR2B subunit gene (GRIN2B) in schizophrenia with universal DNA microarray. Eur J Hum Genet. 2005 Jul;13(7):807-14.. Thornton-Wells TA, Moore JH, Martin ER, Pericak-Vance MA, Haines JL. Confronting complexity in late-onset Alzheimer disease: application of two-stage analysis approach addressing heterogeneity and epistasis. Genet Epidemiol. 2008 Apr;32(3):187-203.. Vilella E, Costas J, Sanjuan J, Guitart M, De Diego Y, Carracedo A, Martorell L, Valero J, Labad A, De Frutos R, Najera C, Molto MD, Toirac I, Guillamat R, Brunet A, Valles V, Perez L, Leon M, de Fonseca FR, Phillips C, Torres M. Association of schizophrenia with DTNBP1 but not with DAO, DAOA, NRG1 and RGS4 nor their genetic interaction. J Psychiatr Res. 2008 Mar;42(4):278-88.. Yasuno K, Ando S, Misumi S, Makino S, Kulski JK, Muratake T, Kaneko N, Amagane H, Someya T, Inoko H, Suga H, ...
NMDA receptors are hetero-oligomers assembled from two typesof subunits, NR1 and NR2. The NR1 subunit is a single geneproduct, whereas the NR2 subunit is encoded by four differentgenes: NR2A-NR2D (147). Native NMDA receptors are thoughtto be heteromultimers containing four or five subunits consistingof two NR1 subunits and two or three NR2 subunits (38). Atmost synapses throughout the central nervous system, NMDA receptorsare composed of NR1 subunits in combination with either NR2Aor NR2B subunits. NR2A and NR2B subunits are ubiquitously distributedthrough the central nervous system and have been shown to undergoa developmental switch in hippocampal and cortical neurons(179). At birth NMDA receptors are composed of NR1/NR2B subunits,and there is a switch from NR2B to NR2A subunits around P7.However, in the LA, a recent study has shown that applicationof the NR2B-selective antagonist ifenprodil blocks the inductionof fear conditioning, suggesting that receptors containingNR2B subunits are present ...
Ultiva® is commonly administered intravenously through standard anaesthesia. IbrutinibIts key constituent is remifentanil, a potent small-performing μ-opioid receptor agonist. Despite the fact that behavioural research in rats counsel that intrathecal administration of remifentanil induces profound analgesia, Ultiva® is not authorized for epidural or intrathecal use in medical observe.The medical formulation of Ultiva® is made up of glycine as an acidic buffer. Glycine is a main inhibitory neurotransmitter in the central anxious system, and is also an significant N-methyl-D-aspartate receptor co-activator with glutamate the latter motion is proposed as a likely mechanism for opioid-induced hyperalgesia. It has also been suggested that remifentanil by itself may well straight boost NMDA receptor-mediated responses in the dorsal horn and market hyperalgesia.Though these results counsel that intrathecal administration of Ultiva® might have contrary professional-nociceptive and anti-nociceptive ...
Ultiva® is commonly administered intravenously through standard anaesthesia. IbrutinibIts key constituent is remifentanil, a potent small-performing μ-opioid receptor agonist. Despite the fact that behavioural research in rats counsel that intrathecal administration of remifentanil induces profound analgesia, Ultiva® is not authorized for epidural or intrathecal use in medical observe.The medical formulation of Ultiva® is made up of glycine as an acidic buffer. Glycine is a main inhibitory neurotransmitter in the central anxious system, and is also an significant N-methyl-D-aspartate receptor co-activator with glutamate the latter motion is proposed as a likely mechanism for opioid-induced hyperalgesia. It has also been suggested that remifentanil by itself may well straight boost NMDA receptor-mediated responses in the dorsal horn and market hyperalgesia.Though these results counsel that intrathecal administration of Ultiva® might have contrary professional-nociceptive and anti-nociceptive ...
Dr. Jonathan Ploski focuses his research on developing clinically effective methods to therapeutically attenuate maladaptive emotional memories. He recently has been examining how the NMDA receptor subunit composition can influence the ability of an existing memory to be modified via reconsolidation updating. Specifically, Dr. Ploski has developed a line of transgenic mice that could specifically overexpress the GluN2A subunit of the NMDA receptor after a memory has been formed. Subsequently, he has found that when the GluN2A subunit is overexpressed, the modification of an existing memory is prevented. Dr. Ploski also has developed a viral-based, inducible CRISPR/Cas9 system for in vivo genome editing that can be used for studies focused on the role of specific genes and behavior. His lab has received a seed grant from the Texas Medical Device Center to develop a viral delivered inducible genome editing system that will facilitate the investigation of how particular genes influence neural ...
In the 1960s and 70s, biochemical and pharmacological evidence was pointing toward glutamate as a synaptic transmitter at a number of distinct receptor classes, known as NMDA and non-NMDA receptors. The field, however, lacked a potent and highly selective antagonist to block these putative postsynaptic receptors. So, the discoveries in the early 1980s of D-AP5 as a selective NMDA receptor antagonist and of its ability to block synaptic events and plasticity were a major breakthrough leading to an explosion of knowledge about this receptor subtype. During the next 10 years, the role of NMDA receptors was established in synaptic transmission, long-term potentiation, learning and memory, epilepsy, pain, among others. Hints at pharmacological heterogeneity among NMDA receptors were followed by the cloning of separate subunits. The purpose of this review is to recognize the important contributions made in the 1980s by Graham L. Collingridge and other key scientists to the advances in our ...
Results-In both in vitro and in vivo ischemia models, glycine at low level exerts deleterious effects in postischemic long-term potentiation and ischemic neuronal injury by modulation of the N-methyl-d-aspartate receptor coagonist site; whereas glycine at high level exerts neuroprotective effects by activation of glycine receptor and subsequent differential regulation of N-methyl-d-aspartate receptor subunit components. Read more. ...
El óxido nítrico (NO) es una molécula con efectos pleyotrópicos en cerebro y sistema vascular. Fisiológicamente, induce la traducción de la subunidad GluN2B del N-methyl D-aspartate receptor (NMDARc) al revertir la represión de su 5untranslated region (5UTR). Este efecto se debe a la activación de la heme regulated eIF2α kinase (HRI) y previene el exceso de GluN2B, especialmente en regiones extrasinápticas, donde desencadena excitotoxicidad. Patológicamente, el NO en un ambiente pro-oxidatvio como el dado en la enfermedad de Alzheimer (AD) reacciona con el anión superóxido produciendo peroxinitrito, y causando entre otros efectos la nitrotirosinación de proteínas. Simultaneamente, las proteínas de pacientes con AD padecen otros procesos oxidativos como la glicación. Por tanto, la albúmina, la proteína plasmática más abundante, en estos pacientes está más nitrotirosinada y glicada, afectando su estructura. La albúmina modificada presenta menos capacidad para tamponar la ...
AbstractIn the present study, a twenty-mer antisense oligonucleotide specific for N-methyl-D-aspartate receptor one (ANR1) was applied to striatal neurons in primary cell culture. The ANR1 was found to be specific and nontoxic. Significant reductions in expression of NR1 mRNA and proteins were resulted after a single dose of ANR1 transcripts. Interestingly, there were reductions in total NR1 proteins but two phosphorylated forms of NR1 proteins at serine 896 and 897 residues were not reduced. There was also no change in the pattern of distribution of NR1 immunoreactivity in the striatal neurons. In addition, significant reductions of NMDA-mediated peak inward current were found after application of a higher concentration of ANR1 (20-100 mu M) by patch clamp recordings. The present results indicate that ANR1 is a useful agent in reducing NMIDA receptor functions. The present data thus provide detailed cellular and molecular mechanisms to explain our previous findings of amelioration of motor ...
Looking for online definition of N-methyl D-aspartate receptor subtype 2C in the Medical Dictionary? N-methyl D-aspartate receptor subtype 2C explanation free. What is N-methyl D-aspartate receptor subtype 2C? Meaning of N-methyl D-aspartate receptor subtype 2C medical term. What does N-methyl D-aspartate receptor subtype 2C mean?
Aggregates of amyloid-beta (Aβ) and tau are hallmarks of Alzheimers disease (AD) leading to neurodegeneration and synaptic loss. While increasing evidence suggests that inhibition of N-methyl-D-aspartate receptors (NMDARs) may mitigate certain aspects of AD neuropathology, the precise role of different NMDAR subtypes for Aβ- and tau-mediated toxicity remains to be elucidated. Using mouse organotypic hippocampal slice cultures from arcAβ transgenic mice combined with Sindbis virus-mediated expression of human wild-type tau protein (hTau), we show that Aβ caused dendritic spine loss independently of tau. However, the presence of hTau was required for Aβ-induced cell death accompanied by increased hTau phosphorylation. Inhibition of NR2B-containing NMDARs abolished Aβ-induced hTau phosphorylation and toxicity by preventing GSK-3β activation but did not affect dendritic spine loss. Inversely, NR2A-containing NMDAR inhibition as well as NR2A-subunit knockout diminished dendritic spine loss ...
Hypertension is major risk factor leading to cerebrovascular pathologies. N-methyl d-aspartate receptors (NMDARs) and renin-angiotensin system are involved in neuronal plasticity, as well as cognitive functions in the hippocampus. In this study, we examined the effects of lisinopril, an ACE inhibitor, on the levels of hippocampal NMDAR subunits; NR2A and NR2B in L-NAME (N-epsilon-nitro-l-arginine Methyl Ester)-induced hypertensive rats. In addition, malondialdehyde (MDA) levels were measured as a marker for lipid peroxidation. Compared with the control group, the MDA level was significantly increased after 8 weeks in the l-NAME-treated group. Rats treated with lisinopril and l-NAME plus lisinopril were found to have significantly decreased hippocampal MDA levels. Regarding the hippocampal concentrations of NR2A and NR2B, there were no statistically significant differences between groups. We demonstrated that lisinopril treatment has no direct regulatory effect on the levels of NR2A and NR2B in ...
Generalizations of NMDA-receptor antagonists to the discriminative stimulus effects of κ-opioid receptor agonists in rats were examined. Phencyclidine, MK-801, and ketamine, non-competitive NMDA-receptor antagonists, generalized to the discriminative stimulus effects of U-50,488H, but not those of TRK-820, whereas (±)-3-(2-carbaxypiperazine-4-yl) propyl-1-phosphonic acid (CPP), a competitive NMDA-receptor antagonist, and ifenprodil, an NR1/NR2B NMDA-receptor antagonist, did not, suggesting that non-competitive NMDA-receptor antagonists possess U-50,488H-like discriminative stimulus effects in rats. Since U-50,488H and phencyclidine both induce aversive effects, our findings indicate that the cue of the discriminative stimulus effects of U-50,488H and non-competitive NMDA-receptor antagonists may be associated with their aversive effects.,br,. ...
Cerebellar granule cells are susceptible to the excitotoxin glutamate, which acts at N-methyl-D-aspartate (NMDA) receptors, as well as the neurotoxin 1-methyl-4-phenylpyridinium ion (MPP+), the active cytotoxic metabolite of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP). Paradoxically, preincubation of cultured cerebellar granule cells with low concentrations of NMDA or glutamate markedly antagonizes the neurotoxicity resulting from subsequent exposure to toxic concentrations of either MPP+ or glutamate. The neuroprotective effects of NMDA and glutamate against MPP+ toxicity are observed at agonist concentrations as low as 1 microM, are blocked by specific NMDA receptor antagonists, and require at least 30 min to develop fully. Moreover, NMDA receptor-mediated neuroprotection is prevented by the RNA synthesis inhibitor actinomycin D or the protein synthesis inhibitor cycloheximide. Thus, in cerebellar granule cells activation of NMDA receptors by glutamate can result in either ...
TY - JOUR. T1 - NMDA receptor blockade prevents the increase in protein kinase C substrate (protein F1) phosphorylation produced by long-term potentiation. AU - Linden, David J.. AU - Wong, Ka L.. AU - Sheu, Fwu Shan. AU - Routtenberg, Aryeh. PY - 1988/8/16. Y1 - 1988/8/16. N2 - Recent evidence has implicated activation of the N-methyl-d-aspartate (NMDA) class of glutamate receptor in the initiation of hippocampal long-term potentiation (LTP), an electrophysiological model of information storage in the brain. A separate line of evidence has suggested that activation of protein kinase C (PKC) and the consequent phosphorylation of it substrates is necessary for the maintenance of the LTP response. To determine if PKC activation is a consequence of NMDA receptor activation during LTP, we applied the NMDA receptor antagonist drug, dl-aminophosphonovalerate (APV) both immediately prior to and following high frequency stimulation, resulting in successful and unsuccessful blockade of LTP initiation, ...
One of the first cognitive dysfunctions to arise with aging is memory loss, affecting an estimated 85% of elderly in the U.S. over the age of 80 with Age Associated Memory Impairment. A common feature in humans and animals experiencing memory loss with aging is the decline in N-methyl-D-aspartate (NMDA) receptorbinding densities in the brain. Variability in the effects of aging on the GluN1 subunit suggests that inflammation may play a role in NMDA receptor aging. The purpose of the present study was to determine the effects of an anti-inflammatory drug, ibuprofen, on spatial long-term & short-term memory and cognitive flexibility in male C57BL/6 mice from four different age groups (5, 14, 20, and 26 months of age at the end of testing). Mice were fed either Ibuprofen (375 ppm) in NIH31 diet or NIH31 diet alone for 6 weeks prior to testing. This dose had been shown to reduce pathology in an Alzheimers disease mouse model. Behavioral testing using the Morris Water Maze showed a significant ...
Alpha-actinin (alpha-actinin-2) is a protein which links the NR1 and NR2B subunits of N-methyl-D-aspartate (NMDA) glutamate receptors to the actin cytoskeleton. Because of the importance of NMDA receptors in modulating the function of the striatum, we have examined the localization of alpha-actinin-2 protein and mRNA in striatal neurons, and its biochemical interaction with NMDA receptor subunits present in the rat striatum. Using an alpha-actinin-2-specific antibody, we found intense immunoreactivity in the striatal neuropil and within striatal neurons that also expressed parvalbumin, calretinin and calbindin. Conversely, alpha-actinin-2 immunoreactivity was not detected in neurons expressing choline acetyltransferase and neuronal nitric oxide synthase. Dual-label in situ hybridization revealed that the highest expression of alpha-actinin-2 mRNA is in substance P-containing striatal projection neurons. The alpha-actinin-2 mRNA is also present in enkephalinergic projection neurons and ...
Abundant evidence suggests that NMDA receptors are involved in the nociceptive responses to formalin. Pretreatment with a competitive NMDA receptor antagonist [e.g., APV[3-amino-5-phosphonovaleric acid] or a noncompetitive NMDA receptor antagonist {e.g.,MK-801, [(+)-5 methyl-10,11-dihydro-5H-dibenzo[a,d]cyclo-hepten-5,10-imine hydrogen maleate], dextromethorphan or ketamine} reduces nociceptive behavioral and/or electrophysiological responses induced by formalin (Coderre and Melzack, 1992; Haley et al., 1990;Yamamoto and Yaksh, 1992; Vaccarino et al., 1993; Hunter and Singh, 1994; Elliott et al., 1995; Shimoyama et al., 1996). The effects of NMDA receptor antagonists are primarily on phase 2 behaviors of the formalin response (Coderre and Melzack, 1992). Phase 2 of the formalin test appears to reflect central sensitization. The barrage of C-fiber inputs produced by formalin most likely activates spinal cord NMDA receptors, which results in the sensitization of dorsal horn neurons. This results ...
We asked whether GABA(A) and NMDA receptors may act in synergy in neonatal hippocampal slices, at a time when GABA exerts a depolarizing action. The GABA(A) receptor agonist isoguvacine reduced the voltage-dependent Mg2+ block of single NMDA channels recorded in cell-attached configuration from P(2-5) CA3 pyramidal neurons and potentiated the Ca2+ influx through NMDA channels. The synaptic response evoked by electrical stimulation of stratum radiatum was mediated by a synergistic interaction between GABA(A) and NMDA receptors. Network-driven Giant Depolarizing Potentials, which are a typical feature of the neonatal hippocampal network, provided coactivation of GABA(A) and NMDA receptors and were associated with spontaneous and synchronous Ca2+ increases in CA3 pyramidal neurons. Thus, at the early stages of development, GABA is a major excitatory transmitter that acts in synergy with NMDA receptors. This provides in neonatal neurons a hebbian stimulation that may be involved in neuronal plasticity and
TY - JOUR. T1 - Insulin promotes rapid delivery of N-methyl-D-aspartate receptors to the cell surface by exocytosis. AU - Skeberdis, Vytenis A.. AU - Lan, Jian Yu. AU - Zheng, Xin. AU - Zukin, R. Suzanne. AU - Bennett, Michael V.L.. N1 - Copyright: Copyright 2007 Elsevier B.V., All rights reserved.. PY - 2001/3/13. Y1 - 2001/3/13. N2 - Insulin potentiates N-methyl-D-aspartate receptors (NMDARs) in neurons and Xenopus oocytes expressing recombinant NMDARs. The present study shows that insulin induced (i) an increase in channel number times open probability (nPo) in outside-out patches excised from Xenopus oocytes, with no change in mean open time, unitary conductance, or reversal potential, indicating an increase in n and/or Po;; (ii) an increase in charge transfer during block of NMDA-elicited currents by the open channel blocker MK-801, indicating increased number of functional NMDARs in the cell membrane with no change in Po;; and (iii) increased NR1 surface expression, as indicated by Western ...
Dopamine and the excitatory amino acids play important roles in the control of motor behavior by the basal ganglia; elucidating the manner in which these transmitter systems interact may provide new therapeutic approaches to the treatment of movement disorders such as Parkinsons disease. The 2-deoxyglucose autoradiographic technique was used to examine the effect of N-methyl-D-aspartate receptor blockade on regional cerebral metabolic responses to D1 and D2 dopamine receptor stimulation in rats with a unilateral 6-hydroxydopamine lesion of the nigrostriatal pathway. The D1 agonist SKF 38393 (5 mg/kg, i.v.) increased glucose utilization markedly in entopeduncular nucleus and substantia nigra pars reticulata ipsilateral to the lesion, while the D2 agonist quinpirole (1 mg/kg, i.v.) had no effect in these striatal output regions. SKF 38393 and quinpirole reduced 2-deoxyglucose uptake to a similar extent in the lateral habenula, a region which receives afferent input from entopeduncular nucleus; quinpirole
Ananth, C., Dheen, S.T., Gopalakrishnakone, P., Kaur, C. (2003). Distribution of NADPH-diaphorase and expression of nNOS, N-Methyl-D-Aspartate receptor (NMDAR1) and Non-NMDA glutamate receptor (GlutR2) genes in the neurons of the hippocampus after domoic acid-induced lesions in adult rats. Hippocampus 13 (2) : 260-272. [email protected] Repository. https://doi.org/10.1002/hipo. ...
TY - JOUR. T1 - Rapid, experience-dependent expression of synaptic NMDA receptors in visual cortex in vivo. AU - Quinlan, Elizabeth M.. AU - Philpot, Benjamin D.. AU - Huganir, Richard L.. AU - Bear, Mark F.. PY - 1999/4/1. Y1 - 1999/4/1. N2 - Sensory experience is crucial in the refinement of synaptic connections in the brain during development. It has been suggested that some forms of experience-dependent synaptic plasticity in vivo are associated with changes in the complement of postsynaptic glutamate receptors, although direct evidence has been lacking. Here we show that visual experience triggers the rapid synaptic insertion of new NMDA receptors in visual cortex. The new receptors have a higher proportion of NR2A subunits and, as a consequence, different functional properties. This effect of experience requires NMDA receptor activation and protein synthesis. Thus, rapid regulation of post- synaptic glutamate receptors is one mechanism for developmental plasticity in the brain. Changes in ...
Experimental and clinical studies showed that intraoperative infusionof remifentanil has been associated with postoperative hyperalgesia. Previous reports suggested that spinal N-methyl-D-aspartate (NMDA) receptors may contribute to the development and maintenance of opioid-induced hyperalgesia. In the present study, we used a rat model of postoperative pain to investigate the role of tyrosine phosphorylation of NMDA receptor 2B (NR2B) subunit in spinal cord in the postoperative hyperalgesia induced by remifentanil and the intervention of pretreatment with ketamine. Intraoperative infusion of remifentanil (0.04 mg/kg, subcutaneous) significantly enhanced mechanical allodynia and thermal hyperalgesia induced by the plantar incision during the postoperative period (each lasting between 2 h and 48 h), which was attenuated by pretreatment with ketamine (10 mg/kg, subcutaneous). Correlated with the pain behavior changes, immunocytochemical and western blotting experiments in our study revealed that there was
The BDNF secretion can be either constitutive or, more frequently, regulated by stimuli.32 This activity-dependent secretion, a feature characteristic of BDNF and not of any other neurotrophin or growth factor,33 may be an important factor in mood regulation. Along with slow effects that require protein synthesis, BDNF exerts rapid signaling events that regulate synaptic plasticity.34 For example, inducing phosphorylation of synapsin and thereby increasing glutamate and GABA release.35 BDNF can also increase ion influx through N-methyl-D-aspartate receptors and then synaptic strength.36 Thus, BDNF is able to regulate synaptic plasticity and recent findings suggest that mood disorders would be associated with alterations in information processing within neural networks.37 A large proportion of neuronal BDNF is secreted in the pro-form (proBDNF) which is subsequently converted to the mature form (mBDNF) by endoproteolytic cleavage.38 Lee et al.39 suggested that the extracellular conversion from ...
Although the importance of NMDARs as a therapeutic target for certain types of neuropathic pain has been well recognized, very few studies have directly examined changes in NMDAR activity in the spinal dorsal horn in different neuropathic pain conditions. We found that nerve injury induced a substantial increase in the amplitudes of NMDAR-EPSCs and postsynaptic NMDAR currents elicited by NMDA puff application in spinal lamina II neurons 3 weeks, but not 3 and 7 days, after SNL. Interestingly, we found that the postsynaptic NMDAR currents were much smaller in lamina I than in lamina II neurons and that nerve injury had no significant effect on NMDAR activity of lamina I neurons. These data indicate that nerve injury-induced increases in postsynaptic NMDAR activity in the spinal dorsal horn are time dependent and lamina specific. By analyzing the decay time of NMDAR-EPSCs and using selective GluN2A and GluN2B blockers, we showed that increased NMDAR activity of lamina II neurons by nerve injury is ...
Cultures of fetal hippocampal neurons were prepared according to the previously described techniques (MacDonald et al., 1989). Briefly, timed-pregnant mice were killed by cervical dislocation. Fetuses were removed, and hippocampi were microdissected and placed in cold Hanks solution. The hippocampi were then mechanically dissociated by trituration and plated in 35-mm, collagen-coated, culture dishes at densities of ,1 × 106 cells/ml. The cells were grown in dissociated tissue culture using standard techniques. The cultures were used for electrophysiological recordings 12-17 days after plating. The culture medium was replaced with extracellular solution before recording.. Acutely isolated hippocampal neurons were obtained as described previously (Jarvis et al., 1997). Rats (approximately 2 weeks of age) were anesthetized with halothane and killed by decapitation using a guillotine. The whole brain was removed and placed in cold extracellular solution (see below for composition). Hippocampi were ...
Hippocampal long-term potentiation (LTP), a long-lasting increase in synaptic efficacy, is the molecular basis for learning and memory. Tetanic stimulation of afferents in the CA1 region of the hippocampus induces glutamate release and activation of glutamate receptors in dendritic spines. A large increase in [Ca2+]i resulting from influx through NMDA receptors leads to constitutive activation of CaM kinase II (CaM KII) . Constitutively active CaM kinase II phosphorylates AMPA receptors, resulting in potentiation of the ionic conductance of AMPA receptors. Early-phase LTP (E-LTP) expression is due, in part, to this phosphorylation of the AMPA receptor. It is hypothesized that postsynaptic Ca2+ increases generated through NMDA receptors activate several signal transduction pathways including the Erk/MAP kinase and cAMP regulatory pathways. The convergence of these pathways at the level of the CREB/CRE transcriptional pathway may increase expression of a family of genes required for late-phase LTP ...
Hippocampal long-term potentiation (LTP), a long-lasting increase in synaptic efficacy, is the molecular basis for learning and memory. Tetanic stimulation of afferents in the CA1 region of the hippocampus induces glutamate release and activation of glutamate receptors in dendritic spines. A large increase in [Ca2+]i resulting from influx through NMDA receptors leads to constitutive activation of CaM kinase II (CaM KII) . Constitutively active CaM kinase II phosphorylates AMPA receptors, resulting in potentiation of the ionic conductance of AMPA receptors. Early-phase LTP (E-LTP) expression is due, in part, to this phosphorylation of the AMPA receptor. It is hypothesized that postsynaptic Ca2+ increases generated through NMDA receptors activate several signal transduction pathways including the Erk/MAP kinase and cAMP regulatory pathways. The convergence of these pathways at the level of the CREB/CRE transcriptional pathway may increase expression of a family of genes required for late-phase LTP ...
TY - JOUR. T1 - Age dependence of homosynaptic non-NMDA mediated long-term depression in field CA1 of rat hippocampal slices. AU - Velíšek, Libor. AU - Moshé, Solomon L.. AU - Stanton, Patric K.. PY - 1993/10/15. Y1 - 1993/10/15. N2 - It has been hypothesized that high levels of presynaptic activity that fail to activate postsynaptic N-methyl-d-aspartate (NMDA) receptors may lead to long-term depression (LTD). Therefore, we tested the ability of high-frequency (50 Hz) synaptic stimulation in the presence of a blocker of NMDA receptors to elicit homosynaptic LTD at Schaffer collateral-CA1 synapses in hippocampal slices from 15-, 30- and 60-day-old rats. In control slices, there were no developmental differences in the incidence of long-term potentiation (LTP) of either EPSP slope or population spike amplitude. However, while NMDA receptor blockade with the specific antagonist d-2-amino-5-phosphonopentanoic acid (AP5; 25 μM) completely eliminated LTP in 30 and 60-day-olds, a significant number ...
To monitor changes in alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionate (AMPA) receptor distribution in living neurons, the AMPA receptor subunit GluR1 was tagged with green fluorescent protein (GFP). This protein (GluR1-GFP) was functional and was transiently expressed in hippocampal CA1 neurons. In dendrites visualized with two-photon laser scanning microscopy or electron microscopy, most of the GluR1-GFP was intracellular, mimicking endogenous GluR1 distribution. Tetanic synaptic stimulation induced a rapid delivery of tagged receptors into dendritic spines as well as clusters in dendrites. These postsynaptic trafficking events required synaptic N-methyl-D-aspartate (NMDA) receptor activation and may contribute to the enhanced AMPA receptor-mediatedtransmission observed during long-term potentiation and activity-dependent synaptic maturation.. ...
The aim of the present thesis was firstly to investigate whether the behavioural deficit resulting from NMDA receptor blockade reflects a genuine learning impairment, rather than a disturbance of some other aspect of brain functioning. The behavioural test used was a reference memory task in the watermaze, the learning of which is highly sensitive to hippocampal dysfunction. It has been claimed that he apparent learning deficits caused by the application of NMDA receptor antagonists may be secondary to sensorimotor disturbances, or drug-induced brain damage. Behavioural and histological analysis in the present study was not consistent with either of these two possibilities. However, owing to the fact that NMDA receptor blockade does indeed cause a number of side effects, subsequent experiments investigated the role of a novel class of receptor, the metabotropic glutamate receptor (mGluR), in both LTP and spatial learning. Previous studies have suggested that mGluR activation is necessary for ...
The present study examined the regional differences in dopamine transporter binding sites and NMDA receptor complex binding based on autoradiographic images obtained in postmortem sections of human normal brain tissues. in middle-aged control tissues, high and comparable levels of [H-3]CFT binding were observed in the caudate nucleus, putamen, and accumbens nucleus without significant alteration along the rostrocaudal axis and ventral and dorsal parts of these nuclei. in aging normal brain tissues, dopamine binding sites for [H-3]CFT were significantly reduced in the caudate nucleus, putamen, and accumbens nucleus. L-[H-3]Glutamate, [H-3]MK-801, and [H-3]glycine binding to the NMDA receptor complex was lower in aging brain tissues than in middle-aged controls. Significant correlation did occur between age and [H-3]CFT binding and between age and L-[H-3]glutamate, [H-3]MK-801, and [H-3]glycine binding sites. These results demonstrate that the basal ganglia have age-associated reductions in ...
During cortical development, NMDA receptors (NMDARs) facilitate presynaptic terminal formation, enhance neurotransmitter release, and are required in presynaptic neurons for spike timing-dependent LTD. However, the extent to which NMDARs are found within cortical presynaptic terminals has remained controversial, and the sub-synaptic localization and dynamics of axonal NMDARs are unknown. Here, using live confocal imaging and biochemical purification of presynaptic membranes, we provide strong evidence that NMDARs localize to presynaptic terminals in vitro and in vivo, in a developmentally regulated manner. NR1 and NR2B subunits are found within the active zone membrane, where they could respond to synaptic glutamate release. Surprisingly, NR1 also appears in glutamatergic and GABAergic synaptic vesicles. During synaptogenesis, NR1 is mobile throughout axons - including growth cones and filopodia, structures that are involved in synaptogenesis. Upon synaptogenic contact, NMDA receptors are ...
TY - JOUR. T1 - Neuronal and glial localization of NMDA receptors in the cerebral cortex. AU - Conti, Fiorenzo. AU - Minelli, Andrea. AU - DeBiasi, Silvia. AU - Melone, Marcello. PY - 1997/2. Y1 - 1997/2. N2 - The crucial role of glutamate receptors of the N-methyl-D-aspartate (NMDA) type in many fundamental cortical functions has been firmly established, as has its involvement in several neuropsychiatric diseases, but until recently, very little was known of the anatomical localization of NMDA receptors in the cerebral cortex of mammals. The recent application of molecular biological techniques to the study of NMDA receptors has allowed the production of specific tools, the use of which has much increased our understanding of the localization of NMDA receptors in the cerebral cortex. In particular, immunocytochemical studies on the distribution of cortical NMDA receptors have: 1. Demonstrated the preferential localization of NMDA receptors in dendritic spines, in line with previous work; 2. ...
Deficiency of Insulin-like growth factor (IGF)--1 hormone may contribute to the genesis of cognitive impairment and dementia in the elderly patients. Old age, in the absence of circulating IGF-1, a hormone with a complex role in brain function have linked IGF-1 to an acceleration of neurological diseases(f). Growth hormone and IGF-1 replacement showed to increase neurogenesis, vascular density, and glucose utilization, and alters NMDA receptor subunit composition in brain areas that are implicated in learning and memory, in animal (g)and children(h) studies ...
Pepicelli O, Fedele E, Bonanno G, Raiteri M, Ajmone-Cat MA, Greco A, Levi G, Minghetti L. In vivo activation of N-methyl-D-aspartate receptors in the rat hippocampus increases prostaglandin E2 extracellular levels and triggers lipid peroxidation through cyclooxygenase-mediated mechanisms. Journal of neurochemistry 2002;81(5):1028-1034 ...
Overproduction of VLDL-TG by the liver is a prominent sequel of insulin resistance, obesity, and diabetes1,2,32,33 and leads to dyslipidemia and cardiovascular disease.32,34 We here report, for the first time to our knowledge, that glycine lowers hepatic VLDL-TG secretion via the central nervous system (CNS). Glycine is the smallest nonessential amino acid and a coagonist of the NMDA receptor along with glutamate.29,30 NMDA receptors in the CNS are important for neurotransmission and have critical roles in mechanisms of synaptic plasticity and network synchronization.29 Our current study demonstrates that glycine-induced potentiation of NR1-containing NMDA receptors in the DVC is sufficient to trigger the hepatic vagus and lower VLDL-TG secretion in normal rats.. The NR1 subunit is an obligatory subunit that forms a functional NMDA receptor when combined with either NR2 or NR3 subunits.29 A typical NMDA receptor is a tetramer that most often consists of 2 glycine-binding NR1 subunits and 2 ...
Acute hypertension produced by methamphetamine (MA) is well known, mainly by the enhancement of catecholamine release from sympathetic terminals. However, the central pressor mechanism of the blood-brain-barrier-penetrating molecule remains unclear. We used radio-telemetry and femoral artery cannulation to monitor the mean arterial pressure (MAP) in conscious free-moving and urethane-anesthetized rats, respectively. Expression of Fos protein (Fos) and phosphorylation of N-methyl-D-aspartate receptor subunit GluN1 in the rostral ventrolateral medulla (RVLM) were detected using Western blot analysis. ELISA was carried out for detection of protein kinase C (PKC) activity in the RVLM. MA-induced glutamate release in the RVLM was assayed using in vivo microdialysis and HPLC. Systemic or intracerebroventricular (i.c.v.) administration of MA augments the MAP and increases Fos expression, PKC activity, and phosphorylated GluN1-ser 896 (pGluN1-ser 896) in the RVLM. However, direct microinjection of MA into the
Working on the idea that postsynaptic and presynaptic mechanisms of long-term potentiation (LTP) expression are not inherently mutually exclusive, we have looked for the existence and functionality of presynaptic mechanisms for augmenting transmitter release in hippocampal slices. Specifically, we asked if changes in glutamate release might contribute to the conversion of silent synapses that show N-methyl-D-aspartate (NMDA) responses but no detectable α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) responses, to ones that exhibit both. Here, we review experiments where NMDA receptor responses provided a bioassay of cleft glutamate concentration, using opposition between peak [glu]cleft and a rapidly reversible antagonist, L-AP5. We discuss findings of a dramatic increase in peak [glu]cleft upon expression of pairing-induced LTP (Choi). We present simulations with a quantitative model of glutamatergic synaptic transmission that includes modulation of the presynaptic fusion pore, ...
NMDA receptors are calcium ion channels that function at the postsynaptic side of excitatory synapses in the central nervous system. NMDA receptors are thought to be tetrameric in structure, composed of two NR1 subunits and two NR2 subunits. It is established that the NMDA receptors function in synaptic plasticity is largely mediated by the NR2 intracellular C-terminal domain, which interacts directly and indirectly with numerous postsynaptic signalling molecules (Sprengel et al 98, Migaud et al 98, Husi et al 00). The purpose of this study was to address questions of evolutionary conservation of the NR2 C-terminal domain and structural properties. Ryan et als study provides two main insights. The first was based on comparisons of the length of the NR2 C-terminus between paralogues and across species. Through simple amino acid sequence alignments of NR2 orthologues it became clear that the NR2 C-terminus profoundly differs in size between vertebrates and invertebrates, with vertebrates ...
N-Methyl-D-aspartic acid or N-Methyl-D-aspartate (NMDA) is an amino acid derivative that acts as a specific agonist at the NMDA receptor mimicking the action of glutamate, the neurotransmitter which normally acts at that receptor. Unlike glutamate, NMDA only binds to and regulates the NMDA receptor and has no effect on other glutamate receptors (such as those for AMPA and kainate). NMDA receptors are particularly important when they become overactive during withdrawal from alcohol as this causes symptoms such as agitation and, sometimes, epileptiform seizures. NMDA is a water-soluble synthetic substance that is not normally found in biological tissue. It was first synthesized in the 1960s. NMDA is an excitotoxin (it kills nerve cells by over-exciting them); this trait has applications in behavioral neuroscience research. The body of work utilizing this technique falls under the term lesion studies. Researchers apply NMDA to specific regions of an (animal) subjects brain or spinal cord and ...
Nitric oxide (NO) has long been implicated in the generation of long-term potentiation (LTP) and other types of synaptic plasticity, a role for which the intimate coupling between NMDA receptors (NMDARs) and the neuronal isoform of NO synthase is likely to be instrumental in many instances. While many types of synaptic plasticity depend on NMDA receptors, others do not, an example of which is LTP triggered by opening of L-type voltage-gated Ca2+ channels (L-VGCCs) in postsynaptic neurons. In CA3-CA1 synapses in the hippocampus, NMDAR-dependent LTP appears to be primarily expressed postsynaptically whereas L-VGCC-dependent LTP, which often coexists with NMDAR-dependent LTP, appears mainly to reflect enhanced presynaptic transmitter release. Since NO is an excellent candidate as a retrograde messenger mediating post-to-presynaptic signaling, we sought to determine if NO functions in L-VGCC-dependent LTP in mouse CA3-CA1 synapses. When elicited by a burst type of stimulation with NMDARs and the associated
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TY - JOUR. T1 - Stability of surface NMDA receptors controls synaptic and behavioral adaptations to amphetamine. AU - Mao, Li Min. AU - Wang, Wei. AU - Chu, Xiang Ping. AU - Zhang, Guo Chi. AU - Liu, Xian Yu. AU - Yang, Yuan Jian. AU - Haines, Michelle. AU - Papasian, Christopher J.. AU - Fibuch, Eugene E.. AU - Buch, Shilpa. AU - Chen, Jian Guo. AU - Wang, John Q.. PY - 2009/5/1. Y1 - 2009/5/1. N2 - Plastic changes in glutamatergic synapses that lead to endurance of drug craving and addiction are poorly understood. We examined the turnover and trafficking of NMDA receptors and found that chronic exposure to the psychostimulant amphetamine (AMPH) induced selective downregulation of NMDA receptor NR2B subunits in the confined surface membrane pool of rat striatal neurons at synaptic sites. This downregulation was a long-lived event and was a result of the destabilization of surface-expressed NR2B caused by accelerated ubiquitination and degradation of crucial NR2B-anchoring proteins by the ...
Drug discrimination studies in rats and monkeys with competitive N-methyl-D-aspartate (NMDA) antagonists an training drugs have shown that these drugs typically cross-substitute for each other, whereas phencyclidine (PCP)-like NMDA channel blockers produce partial, if any, substitution. In the present study, rats and squirrel monkeys were trained to discriminate the
The NMDA subtype of ionotropic glutamate receptors has been implicated in the activity-dependent modification of synaptic efficacy in the mammalian brain. Here we describe a cDNA isolated from Drosophila melanogaster which encodes a putative invertebrate NMDA receptor protein (DNMDAR-I). The deduced …
A series of 2-substituted 3,4-dihydro-2H-1,2-benzothiazine-3-carboxylic acid 1,1-dioxides were synthesized and evaluated for their affinity to the glycine binding site of the N-methyl-d-aspartate (NMDA) receptor. The binding affinity was determined by the displacement of radioligand [(3)H]MDL-105,519 from rat cortical membrane preparations. The most attractive structures in the search for prospective NMDA receptor ligands were identified to be 2-arylcarbonylmethyl substituted 3,4-dihydro-2H-1,2-benzothiazine-3-carboxylic acid 1,1-dioxides. It has been demonstrated for the first time that the replacement of NH group in the ligand by sp(3) CH2 is tolerated. This finding may pave the way for previously unexplored approaches for designing new ligands of the NMDA receptor.
A budget friendly reagent kit from Alomone Labs. Contains a specific NMDA Receptor 2B antibody & biologically active NR2B agonists & antagonists. Lyophilized powder. Economical. Worldwide shipping at room temperature. Your top supplier for glutamate receptor research!
TY - JOUR. T1 - Leitmotifs in the biochemistry of LTP induction. T2 - Amplification, integration and coordination. AU - Dineley, Kelly T.. AU - Weeber, Edwin J.. AU - Atkins, Coleen. AU - Adams, J. Paige. AU - Anderson, Anne E.. AU - Sweatt, J. David. PY - 2001/6/4. Y1 - 2001/6/4. N2 - Hippocampal long-term potentiation (LTP) is a robust and long-lasting form of synaptic plasticity that is the leading candidate for a cellular mechanism contributing to mammalian learning and memory. Investigations over the past decade have revealed that the biochemistry of LTP induction involves mechanisms of great subtlety and complexity. This review highlights themes that have emerged as a result of our increased knowledge of the signal transduction pathways involved in the induction of NMDA receptor-dependent LTP in area CA1 of the hippocampus. Among these themes are signal amplification, signal integration and signal coordination. Here we use these themes as an organizing context for reviewing the profusion ...
Dennis Liotta, Ph.D., is the Samuel Candler Dobbs Professor of Chemistry at Emory University where he has been a faculty member for more than 25 years. He is a renowned organic and medicinal chemist and the author of approximately 200 publications and patents.Dr. Liottas research has focused on the discovery and development of novel antiviral and anticancer agents. Stephen Traynelis, Ph.D., isa professor of pharmacology at Emory University School of Medicine, where he has been a faculty member since 1994 and author of more than 300 papers, abstracts and patents. He is an expert on NMDA receptor activation and modulation ...
Several receptors directly interact with ethanol to promote a cascade of signaling. N-methyl-D-aspartate (NMDA) receptors are ... Ethanol sensitivity of recombinant human N-methyl-D-aspartate receptors. Neurochem Int. 38, 333-340. Nagy, J. (2004). The NR2B ... Another family of receptors, metabotropic glutamate receptors (mGluR), may also contribute by activating MAPK pathways and ... In chronic ethanol users, ethanol binds to GABA receptors causing the down-regulation of GABA receptors; which are now less ...
Mathiesen O, Imbimbo BP, Hilsted KL, Fabbri L, Dahl JB (August 2006). "CHF3381, a N-methyl-D-aspartate receptor antagonist and ... August 2003). "Antinociceptive activity of the N-methyl-D-aspartate receptor antagonist N-(2-Indanyl)-glycinamide hydrochloride ... a putative N-methyl-D-aspartate receptor antagonist". NeuroReport. 13 (16): 2071-4. doi:10.1097/00001756-200211150-00016. PMID ... See also: Receptor/signaling modulators • Adrenergics • Dopaminergics • Melatonergics • Serotonergics • Monoamine reuptake ...
January 2007). "Paraneoplastic Anti-N-methyl-D-aspartate Receptor Encephalitis Associated with Ovarian Teratoma". Ann. Neurol. ... anti-NMDA receptor encephalitis, and polymyositis. The following diseases manifest by means of mucocutaneous dysfunction: ...
"Calmodulin mediates calcium-dependent inactivation of N-methyl-D-aspartate receptors". Neuron. 21 (2): 443-53. doi:10.1016/ ... "Interactions of calmodulin and alpha-actinin with the NR1 subunit modulate Ca2+-dependent inactivation of NMDA receptors". The ... "Competitive binding of alpha-actinin and calmodulin to the NMDA receptor". Nature. 385 (6615): 439-42. doi:10.1038/385439a0. ... "Competitive binding of alpha-actinin and calmodulin to the NMDA receptor". Nature. 385 (6615): 439-42. doi:10.1038/385439a0. ...
"Synthesis and N-Methyl-d-aspartate (NMDA) Receptor Activity of Ketamine Metabolites". Organic Letters. 19 (17): 4572-4575. doi: ... support for hyperglutamatergic effects of N-methyl-D-aspartate receptor antagonists". Arch Gen Psychiatry. 57 (3): 270-6. doi: ... "Multiple mechanisms of ketamine blockade of N-methyl-D-aspartate receptors". Anesthesiology. 86 (4): 903-17. doi:10.1097/ ... of NMDA receptors in the brain results in an activation of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors (AMPA ...
... hydroxycholesterol is a potent allosteric modulator of N-methyl-D-aspartate receptors". J. Neurosci. 33 (44): 17290-300. doi: ... "Different oxysterols have opposing actions at N-methyl-D-aspartate receptors". Neuropharmacology. 85: 232-42. doi:10.1016/j. ... GABAA receptor positive allosteric modulator SGE-516 - GABAA receptor positive allosteric modulator SGE-872 - GABAA receptor ... GABAA receptor negative allosteric modulator, NMDA receptor positive allosteric modulator, sigma-1 receptor agonist, TRPM3 ...
N-methyl-D-aspartate (NMDA) receptors are a class of ionotropic glutamate receptors. NMDA channel has been shown to be involved ... "Entrez Gene: GRIN2D glutamate receptor, ionotropic, N-methyl D-aspartate 2D". Kurschner C, Yuzaki M (Sep 1999). "Neuronal ... Pittaluga A, Pattarini R, Severi P, Raiteri M (1996). "Human brain N-methyl-D-aspartate receptors regulating noradrenaline ... "HIV-1 Tat induces neuronal death via tumor necrosis factor-alpha and activation of non-N-methyl-D-aspartate receptors by a ...
"Nonpsychotropic cannabinoid acts as a functional N-methyl-D-aspartate receptor blocker". Proceedings of the National Academy of ... Unlike other cannabinoid derivatives, HU-211 does not act as a cannabinoid receptor agonist, but instead has NMDA antagonist ...
N-methyl-D-aspartate (NMDA) receptors are a class of ionotropic glutamate receptors. The NMDA receptor channel has been shown ... Glutamate [NMDA] receptor subunit epsilon-2, also known as N-methyl D-aspartate receptor subtype 2B (NMDAR2B or NR2B), is a ... "Entrez Gene: GRIN2B glutamate receptor, ionotropic, N-methyl D-aspartate 2B". Yoshimura Y, Ohmura T, Komatsu Y (July 2003). " ... Adams SL, Foldes RL, Kamboj RK (January 1995). "Human N-methyl-D-aspartate receptor modulatory subunit hNR3: cloning and ...
N-methyl-D-aspartate (NMDA) receptors are a class of ionotropic glutamate receptors. NMDA channel has been shown to be involved ... "Entrez Gene: GRIN2A glutamate receptor, ionotropic, N-methyl D-aspartate 2A". Hamza TH, Chen H, Hill-Burns EM, Rhodes SL, ... Foldes RL, Adams SL, Fantaske RP, Kamboj RK (1994). "Human N-methyl-D-aspartate receptor modulatory subunit hNR2A: cloning and ... Ma J, Zhang GY (September 2003). "Lithium reduced N-methyl-D-aspartate receptor subunit 2A tyrosine phosphorylation and its ...
Brandt MR, Cummons TA, Potestio L, Sukoff SJ, Rosenzweig-Lipson S (June 2005). "Effects of the N-methyl-D-aspartate receptor ... August 2004). "Characterization of two novel N-methyl-D-aspartate antagonists: EAA-090 (2-[8,9-dioxo-2,6-diazabicyclo [5.2.0] ... a potent N-methyl-D-aspartate antagonist, via the use of 3-cyclobutene-1,2-dione as an achiral alpha-amino acid bioisostere". ...
Chen BS, Braud S, Badger JD, Isaac JT, Roche KW (June 2006). "Regulation of NR1/NR2C N-methyl-D-aspartate (NMDA) receptors by ... The main receptors associated with PSD-95 are NMDA receptors. The first two PDZ domains of PSD-95 bind to the C-terminus of ... Glutamate receptor interacting protein (GRIP) is a post-synaptic protein that interacts with AMPA receptors in a fashion ... When researchers noticed apparent structural homology between the C-termini of AMPA receptors and NMDA receptors, they ...
Kleckner NW, Glazewski JC, Chen CC, Moscrip TD (May 1999). "Subtype-Selective Antagonism of N-Methyl-D-aspartate Receptors by ... Harty TP, Rogawski MA (March 2000). "Felbamate Block of Recombinant N-Methyl-D-aspartate Receptors: Selectivity for the NR2B ... Opposing Effects on N-Methyl-D-aspartate and Gamma-Aminobutyric Acid A Receptors". Annals of Neurology. 35 (2): 229-34. doi: ... "Felbamate Block of the N-Methyl-D-aspartate Receptor". The Journal of Pharmacology and Experimental Therapeutics. 273 (2): 878- ...
... s act as potent and specific antagonists of the N-methyl-D-aspartate receptor (NMDAR).[1] They are the only naturally ... "Novel conantokins from Conus parius venom are specific antagonists of N-methyl-D-aspartate receptors". The Journal of ... "Conantokin G is an NR2B-selective competitive antagonist of N-methyl-D-aspartate receptors". Molecular Pharmacology. 58 (3): ... a novel peptide antagonist to the N-methyl-D-aspartic acid (NMDA) receptor". Neuroscience Letters. 118 (2): 241-4. doi:10.1016/ ...
... a new neuroprotective agent acting at the N-methyl-D-aspartate receptor". CNS Drug Reviews. 7 (2): 172-98. doi:10.1111/j.1527- ... With the use of this drug, motor skills have significantly improved upon use, as it is the antagonist to the NMDA receptor. ... Gacyclidine (GK-11) is a psychoactive drug which acts as a dissociative via functioning as a non-competitive NMDA receptor ... "The search for TCP analogues binding to the low affinity PCP receptor sites in the rat cerebellum". Eur. J. Med. Chem. 34 (2): ...
N-methyl-D-aspartate (NMDA) receptors are a class of ionotropic glutamate receptors. NMDA channel has been shown to be involved ... "Entrez Gene: GRIN2C glutamate receptor, ionotropic, N-methyl D-aspartate 2C". Lim IA, Hall DD, Hell JW (Jun 2002). "Selectivity ... Pittaluga A, Pattarini R, Severi P, Raiteri M (1996). "Human brain N-methyl-D-aspartate receptors regulating noradrenaline ... "The human N-methyl-D-aspartate receptor 2C subunit: genomic analysis, distribution in human brain, and functional expression". ...
Reynolds IJ, Miller RJ (1989). "Ifenprodil is a novel type of N-methyl-D-aspartate receptor antagonist: interaction with ... "Neurosteroid modulation of N-methyl-d-aspartate receptors: Molecular mechanism and behavioral effects". Steroids. 76 (13): 1409 ... NMDA receptors are multimeric ionotropic glutamate receptors composed of four subunits. GluN1 is obligate for functional ... Ifenprodil is an inhibitor of the NMDA receptor, specifically of GluN1 (glycine-binding NMDA receptor subunit 1) and GluN2B ( ...
... s can cause an autoimmune illness called N-methyl-D-aspartate (NMDA) receptor encephalitis. In this condition, the ... "N-methyl-D-aspartate receptor antibody production from germinal center reactions: Therapeutic implications". Annals of ... condition where ovarian teratomas cause encephalitis associated with antibodies against the N-methyl-D-aspartate receptor ... teratomas may contain B cells with NMDA-receptor specificities. After surgery, a risk exists of regrowth in place, or in nearby ...
N-methyl-D-aspartate receptor antagonist desegregates eye-specific stripes. Cline HT, Debski EA, Constantine-Paton M. Proc Natl ... Using this system, she and her colleagues demonstrated the importance of NMDA receptors in development plasticity. She ...
Lau LF, Huganir RL (1995). "Differential tyrosine phosphorylation of N-methyl-D-aspartate receptor subunits". J Biol Chem. 270 ... The major excitatory neurotransmitter receptors in the central nervous system are the glutamate receptors. These receptors can ... association of growth factor with receptor dimerization of receptor and autophosphorylation of receptor tyrosine kinase (RTK) ... Receptor tyrosine kinases are type I transmembrane proteins possessing an N-terminal extracellular domain, which can bind ...
... a novel NR2B subunit antagonist of the N-methyl-D-aspartate receptor, on the volume of ischemic brain damage off cytotoxic ... "Functional consequences of NR2 subunit composition in single recombinant N-methyl-D-aspartate receptors". Proceedings of the ... an antagonist of NR2B subunit-containing N-methyl-d-aspartate receptors". Experimental Neurology. 163 (1): 239-43. doi:10.1006/ ... a potent new neuroprotectant which blocks N-methyl-D-aspartate responses". Journal of Medicinal Chemistry. 38 (16): 3138-45. ...
Damage has also been shown to be mediated by N-methyl-D-aspartate receptors. Oligodendrocyte dysfunction may also be implicated ... "PDGF receptors in the rat CNS: during late neurogenesis, PDGF alpha-receptor expression appears to be restricted to glial cells ... Káradóttir, R.; D. Attwell (14 April 2007). "Neurotransmiter receptors in the life and death of oligodendrocytes". Neuroscience ... and the platelet-derived growth factor-alpha receptor subunit (PDGF-alphaR). Mature oligodendrocytes are broadly classified ...
1998). "HIV-1 Tat induces neuronal death via tumor necrosis factor-alpha and activation of non-N-methyl-D-aspartate receptors ... "Entrez Gene: GRIN3B glutamate receptor, ionotropic, N-methyl-D-aspartate 3B". Schröder HC, Perovic S, Kavsan V, et al. (1998 ... 1999). "Evidence of HIV type 1 glycoprotein 120 binding to recombinant N-methyl-D-aspartate receptor subunits expressed in a ... 1995). "Human immunodeficiency virus type 1 tat activates non-N-methyl-D-aspartate excitatory amino acid receptors and causes ...
It acts as an N-methyl-D-aspartate receptor (NMDAR) antagonist. The compound also has low affinity for opioid receptors, ... and l-isomers of methadone bind to the non-competitive site on the N-methyl-D-aspartate (NMDA) receptor in rat forebrain and ...
"A quantitative review of the postmortem evidence for decreased cortical N-methyl-D-aspartate receptor expression levels in ... "Molecular evidence of N-methyl-D-aspartate receptor hypofunction in schizophrenia". Molecular Psychiatry. 18 (11): 1185-92. doi ... "Interleukin 1 receptor antagonist and soluble tumor necrosis factor receptor 1 are associated with general severity and ... In particular, the expression of mRNA for the NR1 receptor subunit, as well as the protein itself is reduced in the prefrontal ...
This gene encodes a subunit of the N-methyl-D-aspartate (NMDAR) receptors, which belong to the superfamily of glutamate- ... "Entrez Gene: GRIN3A glutamate receptor, ionotropic, N-methyl-D-aspartate 3A". Schröder HC, Perovic S, Kavsan V, Ushijima H, ... Pittaluga A, Pattarini R, Severi P, Raiteri M (1996). "Human brain N-methyl-D-aspartate receptors regulating noradrenaline ... "HIV-1 Tat induces neuronal death via tumor necrosis factor-alpha and activation of non-N-methyl-D-aspartate receptors by a ...
The protein encoded by this gene is a critical subunit of N-methyl-D-aspartate receptors, members of the glutamate receptor ... 1999). "N-methyl-D-aspartate and dopamine receptor involvement in the modulation of locomotor activity and memory processes". ... "Entrez Gene: GRIN1 glutamate receptor, ionotropic, N-methyl D-aspartate 1". Lin JW, Wyszynski M, Madhavan R, et al. (1998). " ... 1993). "Molecular cloning and chromosomal localization of the key subunit of the human N-methyl-D-aspartate receptor". J. Biol ...
Ma MC, Huang HS, Chen YS, Lee SH (Nov 2008). "Mechanosensitive N-methyl-D-aspartate receptors contribute to sensory activation ... "D-serine is an endogenous ligand for the glycine site of the N-methyl-D-aspartate receptor". Proceedings of the National ... D-serine is a potent agonist at the glycine site (NR1) of the NMDA-type glutamate receptor (NMDAR). For the receptor to open, ... Had D amino acids been discovered in humans sooner, the glycine site on the NMDA receptor might instead be named the D-serine ...
Lu Y, France CP, Woods JH (November 1992). "Tolerance to the cataleptic effect of the N-methyl-D-aspartate (NMDA) receptor ... July 1988). "CGS 19755, a selective and competitive N-methyl-D-aspartate-type excitatory amino acid receptor antagonist". The ... 1990). "CGS 19755: a novel competitive N-methyl-D-aspartate (NMDA) receptor antagonist with anticonvulsant, anxiolytic and anti ... a competitive antagonist at N-methyl-D-aspartate receptors". The Journal of Pharmacology and Experimental Therapeutics. 250 (2 ...
"Entrez Gene: GRINL1A glutamate receptor, ionotropic, N-methyl D-aspartate-like 1A". Maruyama K, Sugano S (1994). "Oligo-capping ... NMDA receptor GRCh38: Ensembl release 89: ENSG00000255529 - Ensembl, May 2017 GRCm38: Ensembl release 89: ENSMUSG00000032199 - ... Roginski RS, Mohan Raj BK, Finkernagel SW, Sciorra LJ (2001). "Assignment of an ionotropic glutamate receptor-like gene ( ...
"Antihyperalgesic and analgesic properties of the N-methyl-D-aspartate (NMDA) receptor antagonist neramexane in a human ... One major pathway being through stimulation of the nociceptin receptor,[8][9][10] and blocking this receptor may therefore be a ... De Kock MF, Lavand'homme PM (March 2007). "The clinical role of NMDA receptor antagonists for the treatment of postoperative ... Chronic hyperstimulation of opioid receptors results in altered homeostasis of pain signalling pathways in the body with ...
... also examined how mild exercise affected androgen synthesis which in turn causes AHN activation of N-methyl-D-aspartate (NMDA) ... Receptor/signaling modulators. Androgens and antiandrogens. Estrogen receptor modulators. Progesterone receptor modulators. ... 19-Nortestosterone derivatives: 7α-Methyl-19-norandrostenedione (MENT dione, trestione). *11β-Methyl-19-nortestosterone *11β- ... increase beta adrenergic receptors while decreasing alpha adrenergic receptors- which results in increased levels of ...
... a positive allosteric modulator at the N-methyl-D-aspartate receptor" (abstract). Molecular Pharmacology. 40 (3): 333-6. PMID ... The GABAA receptors are made up of subunits which form a receptor complex. Humans have 19 receptor subunits and are classified ... See also: Receptor/signaling modulators • GABA receptor modulators • GABA metabolism/transport modulators ... and sigma receptors.[18] The neurosteroid Progesterone (PROG) that activates progesterone receptors expressed in peripheral and ...
... subunit of the N-methyl-D-aspartate receptor". The Journal of Biological Chemistry. 276 (1): 693-99. doi:10.1074/jbc.M008085200 ... "PSD-95 promotes Fyn-mediated tyrosine phosphorylation of the N-methyl-D-aspartate receptor subunit NR2A". Proceedings of the ... The TrkB receptor is encoded by the NTRK2 gene and is member of a receptor family of tyrosine kinases that includes TrkA and ... receptor binding. • neurotrophin TRKB receptor binding. • growth factor activity. • GO:0001948 protein binding. ...
"Selective impairment of learning and blockade of long-term potentiation by an N-methyl-D-aspartate receptor anatagonist, AP5". ... The function of NMDA receptors varies according to the subregion of the hippocampus. NMDA receptors are required in the CA3 of ... Spatial learning requires both NMDA and AMPA receptors, consolidation requires NMDA receptors, and the retrieval of spatial ... Blockade of the NMDA receptors prevents induction of long-term potentiation and impairs spatial learning. The CA3 of the ...
Indirect/downstream NO modulators: ACE inhibitors/AT-II receptor antagonists (e.g., captopril, losartan) ... Nω-Methyl-L-arginine (L-NMA). *Nω-Propyl-L-arginine (L-NPA) ... Aspartate. *Glutamate. *Homocysteic acid (L-HCA). * ... is also identified as a potential small molecule antagonist that disrupts this interaction between S100P and RAGE receptor.[15] ...
... and N-methyl-D-aspartate). Inhibitory effects on 5-HT, norepinephrine, and dopamine transporters are weak.[68] Lamotrigine is a ... σ receptors, IC50=145μM. Pharmacokinetics[edit]. The pharmacokinetics of lamotrigine follow first-order kinetics, with a half- ... NMDA receptor antagonists (e.g., ketamine, dextromethorphan, methadone). *Opioids (e.g., hydrocodone, morphine, oxycodone, ... It also blocks L-, N-, and P-type calcium channels and has weak 5-hydroxytryptamine-3 (5-HT3) receptor inhibition. These ...
The major ionotropic glutamine receptors include the N-methyl-D-aspartate (NMDA) and alpha-amino-3-hydroxy-5-methylisoxazole-4- ... The GABAB receptor has been found to be the most important of the three receptors for this disorder as it is vital in both GABA ... Studies have shown that alterations of both the GABAA receptor and the GABAB receptor early in the life of the Aldh5a1-/- mice ... propionic acid (AMPA)/kainite receptor. High levels of GHB have been shown to depress both the NMDA and AMPA/kainite receptor ...
Aspartic acid (aspartate). *DIDS. *Direct blue 71. *Erythro-4-methyl-L-glutamic acid ... See also: Receptor/signaling modulators • Ionotropic glutamate receptor modulators • Metabotropic glutamate receptor modulators ... Specifically, it binds to ionotropic glutamate receptors in the micromolar range, including the AMPA and kainate receptors and ... See also: Receptor/signaling modulators • Ionotropic glutamate receptor modulators • Glutamate metabolism/transport modulators ...
Receptor/signaling modulators. GABA receptor modulators. GABAA receptor positive modulators. Ionotropic glutamate receptor ... "Methyl chloroform". Immediately Dangerous to Life and Health Concentrations (IDLH). National Institute for Occupational Safety ... See also: Receptor/signaling modulators • GABA receptor modulators • GABA metabolism/transport modulators ... The organic compound 1,1,1-trichloroethane, also known as methyl chloroform, is a chloroalkane. This colourless, sweet-smelling ...
Many receptors have a binding site exposed on the cell surface and an effector domain within the cell, which may have enzymatic ... Extremely minor chemical changes such as the addition of a single methyl group to a binding partner can sometimes suffice to ... and threonine from aspartate. If amino acids are present in the environment, microorganisms can conserve energy by taking up ... Lectins typically play a role in biological recognition phenomena involving cells and proteins.[39] Receptors and hormones are ...
Receptor/signaling modulators. GABA receptor modulators. GABAA receptor positive modulators. Ionotropic glutamate receptor ... methyl chloroform), trichloroethylene) ... Aspartic acid (aspartate). *Glutamic acid (glutamate). * ... Like taurine, it also acts as an endogenous neurotransmitter via action on the glycine receptors.[1] ...
"Density of glutamic acid decarboxylase 67 messenger RNA-containing neurons that express the N-methyl-D-aspartate receptor ... Receptor/signaling modulators GABA receptor modulators GABAA receptor positive modulators Glutamate metabolism/transport ... See also: Receptor/signaling modulators • Ionotropic glutamate receptor modulators • Metabotropic glutamate receptor modulators ... Reduced GABA levels increase glutamate levels as a consequence of lower inhibition of subtypes of GABA receptors. Higher ...
The N-methyl-D-aspartate receptor (also known as the NMDA receptor or NMDAR), is a glutamate receptor and ion channel found in ... Activation of NMDA receptors requires binding of glutamate or aspartate (aspartate does not stimulate the receptors as strongly ... Clinical trial number NCT00188383 for "Effects of N-Methyl-D-Aspartate (NMDA)-Receptor Antagonism on Hyperalgesia, Opioid Use, ... Traynelis SF, Cull-Candy SG (May 1990). "Proton inhibition of N-methyl-D-aspartate receptors in cerebellar neurons". Nature. ...
The anticonvulsant MK-801 is a potent N-methyl-D-aspartate antagonist". Proc Natl Acad Sci USA. 83 (18): 7104-8. PMC 386661 . ... NMDA receptor. Reference[уреди]. *^ Foster AC, Fagg GE (1987). „Neurobiology. Taking apart NMDA receptors". Nature. 329 (6138 ... Dizocilpin (INN) (MK-801) je nekompetitivni antagonist N-metil-d-aspartat (NMDA) receptora, glutamatnog receptor. Glutamat je ... Briggs CA, McKenna DG (1996). „Effect of MK-801 at the human alpha 7 nicotinic acetylcholine receptor". Neuropharmacology. 35 ( ...
In addition there is a synergistic effect with endogenous glutamate and N-Methyl-D-aspartate receptor agonists that contribute ... a neurotransmitter in the brain that activates glutamate receptors. Domoic acid has a very strong affinity for these receptors ... The effects of domoic acid have been attributed to several mechanisms, but the one of concern is through glutamate receptors. ... It damages the neurons by activating AMPA and kainate receptors, causing an influx of calcium. Although calcium flowing into ...
The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (also known as AMPA receptor, AMPAR, or quisqualate receptor ... "NMDA receptor activation dephosphorylates AMPA receptor glutamate receptor 1 subunits at threonine 840". J. Neurosci. 27 (48): ... AMPA receptor trafficking to the PSD in response to LTP[edit]. Once AMPA receptors are transported to the perisynaptic region ... AMPA receptors (AMPAR) are both glutamate receptors and cation channels that are integral to plasticity and synaptic ...
Takadera, Tsuneo, Risa Suzuki, and Tetsuro Mohri (1990 "Protection by Ethanol of Cortical Neurons from N-methyl-d-aspartate- ... Dutertre, S., and R. Lewis (2006) "Toxin Insights into Nicotinic Acetylcholine Receptors." Biochemical Pharmacology, 72 (6): ... by Mild and Intense Insults with N-Methyl-D-Aspartate or Nitric Oxide/Superoxide in Cortical Cell Cultures." Proceedings of the ... Blanco, Ana M., Soraya L. Valles, Maria Pascual, and Consuelo Guerri (2005) "Involvement of TLR4/Type I IL-1 Receptor Signaling ...
A transferase is any one of a class of enzymes that enact the transfer of specific functional groups (e.g. a methyl or glycosyl ... Kirsch JF, Eichele G, Ford GC, Vincent MG, Jansonius JN, Gehring H, Christen P (Apr 1984). "Mechanism of action of aspartate ... Braida D, Ponzoni L, Martucci R, Sparatore F, Gotti C, Sala M (May 2014). "Role of neuronal nicotinic acetylcholine receptors ( ... EC 2.5 relates to enzymes that transfer alkyl or aryl groups, but does not include methyl groups. This is in contrast to ...
"Glutathione Is an Endogenous Ligand of Rat Brain N-Methyl-D-Aspartate (NMDA) and 2-Amino-3-Hydroxy-5-Methyl-4- ... See also: Receptor/signaling modulators • Ionotropic glutamate receptor modulators • Glutamate metabolism/transport modulators ... This glutamate in turn acts on mGluR2/3 receptors, and at higher doses of acetylcysteine, mGluR5.[50][51] ... Glutathione also modulates the NMDA receptor by acting at the redox site.[30][49] ...
... is involved in the N-methyl-d-aspartate receptor signaling". Molecular Biology of the Cell. 14 (7): 2921-34. doi:10.1091/mbc. ... ephrin receptor signaling pathway. • filopodium assembly. • T cell costimulation. • blood coagulation. • positive regulation of ... apolipoprotein A-I receptor binding. • GTP-dependent protein binding. • GTPase activity. • mitogen-activated protein kinase ... Fc-gamma receptor signaling pathway involved in phagocytosis. • actin filament organization. • negative regulation of protein ...
16%). The drug also increases the QT interval and liver enzymes (alanine transaminase, aspartate transaminase).[2][6] ... Receptor antagonists. *ERA (Atrasentan). *Retinoid X receptor (Bexarotene). *Sex steroid (Testolactone). Other/ungrouped. * ...
... untranslated regions of the rat N-methyl-D-aspartate receptor 2A gene , revista = Gene , volume = 295 , número = 1 , páxinas = ... and IRAK control glutamate receptor density at the Drosophila NMJ , revista = Neuron , volume = 55 , número = 6 , páxinas = 859 ... Functional organization of the GluR1 glutamate receptor promoter , revista = J. Biol. Chem. , volume = 276 , número = 28 , ... Nuclear factor kappaB controls acetylcholine receptor clustering at the neuromuscular junction , revista = J. Neurosci. , ...
... evidence for N-methyl-D-aspartate-coupled and dopamine reuptake carrier-associated phencyclidine binding sites". Mol. Pharmacol ... Pechnick RN, Bresee CJ, Poland RE (2006). "The role of antagonism of NMDA receptor-mediated neurotransmission and inhibition of ... Amino acid reuptake inhibitor Excitatory amino acid reuptake inhibitor (or glutamate-aspartate reuptake inhibitor) GABA ... and they exert these effects by binding to and activating the transient receptor potential cation channel TRPC6. Activation of ...
... a positive allosteric modulator at the N-methyl-D-aspartate receptor". Molecular Pharmacology. 40 (3): 333-6. PMID 1654510.. ... Receptor/signaling modulators. GABA receptor modulators. GABAA receptor positive modulators. Ionotropic glutamate receptor ... Nuclear receptor activity[edit]. Pregnenolone has been found to act as an agonist of the pregnane X receptor.[13] ... "Transient receptor potential M3 channels are ionotropic steroid receptors in pancreatic beta cells". Nature Cell Biology. 10 ( ...
"7-Chlorokynurenic acid is a selective antagonist at the glycine modulatory site of the N-methyl-D-aspartate receptor complex". ... "Glycine site N-methyl-D-aspartate receptor antagonist 7-CTKA produces rapid antidepressant-like effects in male rats". Journal ...
Banks, P.; Franks, N. P.; Dickinson, R. Competitive inhibition at the glycine site of the N-methyl-D-aspartate receptor ... The diverse actions of volatile and gaseous anesthetics on human-cloned 5-hydroxytryptamine3 receptors expressed in Xenopus ... Tonic inhibitory role of alpha4beta2 subtype of nicotinic acetylcholine receptors on nociceptive transmission in the spinal ...
... central role of N-methyl-D-aspartate receptors in the sensitivity mechanism". Environ. Health Perspect. 111 (12): 1461-4. doi: ...
N-methyl-d-aspartate receptor;. PSC,. postsynaptic current;. EPSC,. excitatory PSC;. IPSC,. inhibitory PSC;. GABA,. γ- ... Modulation of N-methyl-d-aspartate receptor function by glycine transport. Richard Bergeron, Torsten M. Meyer, Joseph T. Coyle ... Modulation of N-methyl-d-aspartate receptor function by glycine transport. Richard Bergeron, Torsten M. Meyer, Joseph T. Coyle ... Modulation of N-methyl-d-aspartate receptor function by glycine transport Message Subject (Your Name) has sent you a message ...
N-methyl-d-aspartate;. NMDAR,. NMDA receptor;. NMDARc,. NMDAR current;. sSC,. superficial layers of the superior colliculus;. ... Developmental loss of miniature N-methyl-d-aspartate receptor currents in NR2A knockout mice. Matthew Townsend, Akira Yoshii, M ... The N-methyl-d-aspartate (NMDA) glutamate receptor (NMDAR), long implicated in developmental plasticity, shows decay time ... In visual pathways, N-methyl-d-aspartate (NMDA) receptors (NMDARs) contain NR1 (GluR ζ1) plus varying proportions of NR2A (GluR ...
... receptor encephalitis. Download Prime PubMed App to iPhone, iPad, or Android ... N-methyl-D-aspartate receptor antibody encephalitis: value of immunomodulatory therapy].. *Pediatric anti-N-methyl-D-aspartate ... AdolescentAnti-N-Methyl-D-Aspartate Receptor EncephalitisBrainChildDiagnosis, DifferentialFemaleHumansImmunologic Factors ... Pediatric anti-N-methyl-D-aspartate receptor encephalitis-clinical analysis and novel findings in a series of 20 patients. ...
N-methyl-D-aspartate receptors (NMDARs) are known for their role in the induction of long-term potentiation (LTP). Here we ... N-methyl-d-aspartate receptors, NMDARs; N-methyl-d-aspartate, NMDA; Short-term potentiation, STP. ... Long-term potentiation and the role of N-methyl-D-aspartate receptors Brain Res. 2015 Sep 24;1621:5-16. doi: 10.1016/j.brainres ... N-methyl-D-aspartate receptors (NMDARs) are known for their role in the induction of long-term potentiation (LTP). Here we ...
The rehabilitation of children with anti-N-methyl-D-aspartate-receptor encephalitis: a case series.. Houtrow AJ1, Bhandal M, ... Anti-N-methyl-D-aspartate (NMDA)-receptor encephalitis is a serious, complex, and potentially fatal disease in children. ... In this case series, we report on six known consecutive pediatric cases of N-methyl-D-aspartate-receptor antibody encephalitis ... Because of the complicated management and extensive rehabilitation needs of children with anti-N-methyl-D-aspartate-receptor ...
Effects of volatile solvents on recombinant N-methyl-D-aspartate receptors expressed in Xenopus oocytes.. Cruz SL1, Balster RL ... 1. We have previously shown that toluene dose-dependently inhibits recombinant N-methyl-D-aspartate (NMDA) receptors at ... Effects of volatile solvents on recombinant N-methyl-D-aspartate receptors expressed in Xenopus oocytes ... Effects of volatile solvents on recombinant N-methyl-D-aspartate receptors expressed in Xenopus oocytes ...
Anti-N-methyl-d-aspartate-receptor (NMDA-R) encephalitis is a new autoimmune disorder, often paraneoplastic in nature, ... anti-NMDA receptor, encephalitis, management, treatment, complications, paraneoplastic ... Anti-N-methyl-d-aspartate-receptor encephalitis: diagnosis, optimal management, and challenges Andrea P Mann,1 Elena ... Anti-N-methyl-D-aspartate-receptor encephalitis: diagnosis, optimal management, and challenges. ...
Anti-N-methyl-D-aspartate receptor encephalitis associated with ovarian immature teratoma. Download Prime PubMed App to iPhone ... Anti-N-methyl-D-aspartate Receptor Encephalitis Associated With Ovarian Immature Teratoma. J Obstet Gynaecol Res. 2011;37(12): ... "Anti-N-methyl-D-aspartate Receptor Encephalitis Associated With Ovarian Immature Teratoma." The Journal of Obstetrics and ... Anti-N-methyl-D-aspartate receptor encephalitis associated with ovarian immature teratoma. J Obstet Gynaecol Res. 2011;37(12): ...
... ... Mohammed Naeem, Hala Al Alem, Ali Al Shehri, and Majed Al-Jeraisy, "Effect of N-Methyl-D-Aspartate Receptor Antagonist ...
Cellular uptake disguises action of L-glutamate on N-methyl-D-aspartate receptors: With an appendix: Diffusion of transported ... 2In slices, the potencies of the weakly (or non-) transported analogues, N-methyl-D-aspartate (NMDA) and kainate (KA) (EC50 = ... T. C. Bellamy, J. Wood, D. A. Goodwin, J. Garthwaite, Rapid desensitization of the nitric oxide receptor, soluble guanylyl ... 3In dissociated cells, L-glutamate was 280 fold more potent (calculated EC50 = 1.7 μM). L- and D-aspartate (calculated EC50 = ...
Pediatric anti-N-methyl-d-aspartate receptor encephalitis-clinical analysis and novel findings in a series of 20 patients. J ... Comparative outcomes in children and adults with anti-N-methyl-d-aspartate (anti-NMDA) receptor encephalitis. J Child Neurol. ... Zhou Y, Liu J, Xiong H. HIV-1 glycoprotein 120 enhancement of N-methyl-d-aspartate NMDA receptor-mediated excitatory ... Paraneoplastic anti-N-methyl-d-aspartate receptor encephalitis associated with ovarian teratoma. Ann Neurol. 2007;61:25-36. ...
Books about Anti N Methyl D Aspartate Receptor Encephalitis , What Should I Read Next?. Register for free to build your own ... Books with the subject: Anti N Methyl D Aspartate Receptor Encephalitis. Up to 20 books are listed, in descending order of ...
... aspartate Receptor-Related Signaling Pathway in the Spinal Cord of Normal Rats ... Effects of Electroacupuncture on N-Methyl-D-aspartate Receptor-Related Signaling Pathway in the Spinal Cord of Normal Rats. ...
Effects of N-Methyl-D-Aspartate (NMDA)-Receptor Antagonism on Hyperalgesia, Opioid Use, and Pain After Radical Prostatectomy. ... C-fibres release glutamate which acts at three receptor types: metabotropic, kainate/AMPA and NMDA. NMDA receptor activation, ... Effects of NMDA-Receptor Antagonism on Hyperalgesia, Opioid Use, and Pain After Radical Prostatectomy in Young and Elderly ... In humans, NMDA-receptor antagonism decreases secondary hyperalgesia subsequent to experimentally-induced pain. ...
... an NMDA receptor (NMDAR) antagonist, had rapid and long-lasting antidepressant effects, there has been increased interest in ... an NMDA receptor (NMDAR) antagonist, had rapid and long-lasting antidepressant effects, there has been increased interest in ... The N-methyl-D-aspartate receptors (NMDARs) are a class of ionotropic glutamate receptors that are widely expressed in the ... 2000). D-serine is an endogenous ligand for the glycine site of the N-methyl-D-aspartate receptor. Proc. Natl. Acad. Sci. U S A ...
Glutamate receptor, ionotropic, N-methyl D-aspartate 2B, genome duplicate bImported. ,p>Information which has been imported ... Cluster: Glutamate receptor, ionotropic, N-methyl D-aspartate 2B, genome duplicate b. 9. ... Cluster: Glutamate receptor, ionotropic, N-methyl D-aspartate 2B, genome duplicate b. 65. ... tr,A2BH14,A2BH14_DANRE Glutamate receptor, ionotropic, N-methyl D-aspartate 2B, genome duplicate b OS=Danio rerio OX=7955 GN= ...
N-Methyl D-aspartate receptors (NMDAR) are ligand-gated ion channels involved in numerous neurological functions, including ... N-Methyl D-aspartate receptors (NMDAR) are ligand-gated ion channels involved in numerous neurological functions, including ... N-Methyl D-aspartate receptors (NMDAR) are ligand-gated ion channels involved in numerous neurological functions, including ... Enzymes Regulating the Homeostasis of Agonists and Antagonists of the N-Methyl D-Aspartate Receptors. ...
Adenosine and anoxia reduce N-methyl-D-aspartate receptor open probability in turtle cerebrocortex. ... Adenosine and anoxia reduce N-methyl-D-aspartate receptor open probability in turtle cerebrocortex. ... Adenosine and anoxia reduce N-methyl-D-aspartate receptor open probability in turtle cerebrocortex. ... Adenosine and anoxia reduce N-methyl-D-aspartate receptor open probability in turtle cerebrocortex. ...
Anti-N-methyl-d-aspartate receptor (NMDAR) encephalitis is a form of autoimmune encephalitis associated with antibodies against ... anti-N-methyl-d-aspartate receptor encephalitis, schizophrenia, differential diagnosis, treatment ... Anti-N-methyl-d-aspartate receptor encephalitis in a patient with a 7-year history of being diagnosed as schizophrenia: ... Anti-N-methyl-d-aspartate receptor encephalitis in a patient with a 7-year history of being diagnosed as schizophrenia: ...
ABSTRACTN-methyl-D-aspartate receptor (NMDA-R) antibody encephalitis is an immune-mediated disorder characterized by the ... ABSTRACT: N-methyl-D-aspartate receptor (NMDA-R) antibody encephalitis is an immune-mediated disorder characterized by the ... Successful Intrathecal Rituximab Administration in Refractory Nonteratoma Anti-N-Methyl-D-Aspartate Receptor Encephalitis: A ...
Human cerebrospinal fluid monoclonal N-methyl-D-aspartate receptor autoantibodies are sufficient for encephalitis pathogenesis ... Anti-N-methyl-D-aspartate receptor (NMDAR) encephalitis is a recently discovered autoimmune syndrome associated with psychosis ... that human cerebrospinal fluid-derived monoclonal NR1 antibodies alone are sufficient to cause neuronal surface receptor ...
1992) Neomycin is an agonist at a polyamine site on the N-methyl-d-aspartate receptor. J Neurochem 59:2087-2093. ... 1994) Sensitivity of the N-methyl-d-aspartate receptor to polyamines is controlled by NR2 subunits. Mol Pharmacol 45:803-809. ... Polyamine-Like Actions of Aminoglycosides at RecombinantN-Methyl-d-Aspartate Receptors. Scott C. Harvey and Phil Skolnick ... Polyamine-Like Actions of Aminoglycosides at RecombinantN-Methyl-d-Aspartate Receptors. Scott C. Harvey and Phil Skolnick ...
... d-Aspartate Receptor Encephalitis With Comorbid Sinus Venous Thrombosis. To the Editor: Anti-N-methyl-d-aspartate (NMDA) ... Neuropsychiatric Presentation of Anti-N-Methyl-d-Aspartate Receptor Encephalitis With Comorbid Sinus Venous Thrombosis. Gagan ... Cardiac sympathetic dysfunction in anti-NMDA receptor encephalitis. Auton Neurosci. 2015;193:142-146. PubMed doi:10.1016/j. ... Anti-NMDA-receptor encephalitis presenting with catatonia and neuroleptic malignant syndrome in patients with intellectual ...
N-methyl-D-aspartate (NMDA) and non-NMDA type glutamate receptors are present on squid giant axon Schwann cells ... N-methyl-D-aspartate (NMDA) and non-NMDA type glutamate receptors are present on squid giant axon Schwann cells ... N-methyl-D-aspartate (NMDA) and non-NMDA type glutamate receptors are present on squid giant axon Schwann cells ... N-methyl-D-aspartate (NMDA) and non-NMDA type glutamate receptors are present on squid giant axon Schwann cells ...
Immature Teratoma Associated With Anti-N-Methyl-D-Aspartate Receptor Encephalitis Yuliya Malayev, DO, MPH; Jared Alberts, MD; ... Anti-N-methyl-D-aspartate-receptor encephalitis: diagnosis, optimal management, and challenges. Ther Clin Risk Manag. 2010; 10 ... N--methyl-D-aspartate (NMDA) receptor encephalitis usually occurs in young, otherwise healthy women.1 Frequently, the diagnosis ... Anti-N-methyl-D-aspartate receptor encephalitis was diagnosed and, with excision and medical management, her symptoms resolved ...
Subtype-selective inhibition of N-methyl-D-aspartate receptors by haloperidol.. V I Ilyin, E R Whittemore, J Guastella, E Weber ... Subtype-selective inhibition of N-methyl-D-aspartate receptors by haloperidol.. V I Ilyin, E R Whittemore, J Guastella, E Weber ... Subtype-selective inhibition of N-methyl-D-aspartate receptors by haloperidol.. V I Ilyin, E R Whittemore, J Guastella, E Weber ... Subtype-selective inhibition of N-methyl-D-aspartate receptors by haloperidol. Message Subject (Your Name) has forwarded a page ...
... more and more medical researchers realized that anti-N-methyl-D-aspartate receptor (NMDAR) encephalitis can be triggered by ... A Case of Anti-N-Methyl-D-Aspartate Receptor Encephalitis Triggered by Herpes Simplex Virus Encephalitis. Xuehong Jin1*# and ... Anti-N-Methyl-D-Aspartate receptor encephalitis is a type of in lammation of brain which can be lethal if remains untreated. ... Here we report a case of a 20-year-old Chinese male student where anti-N-methyl-D-aspartate receptor (NMDAR) encephalitis as ...
Stimulatory and Inhibitory Properties of Aminoglycoside Antibiotics at N-Methyl-d-Aspartate Receptors Takashi Masuko, Tomoko ... Stimulatory and Inhibitory Properties of Aminoglycoside Antibiotics at N-Methyl-d-Aspartate Receptors Takashi Masuko, Tomoko ... Stimulatory and Inhibitory Properties of Aminoglycoside Antibiotics at N-Methyl-d-Aspartate Receptors Takashi Masuko, Tomoko ... The effects of aminoglycoside antibiotics onN-methyl-d-aspartate (NMDA) receptors were studied using voltage-clamp recording of ...
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... receptor antagonist, is frequently used in pediatric general anesthesia. Accumulating evidence from animal experiments has ... Ketamine-induced neuronal damage and altered N-methyl-D-aspartate receptor function in rat primary forebrain culture Toxicol ... Ketamine, a noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist, is frequently used in pediatric general anesthesia ... NMDA receptors regulate channels that are highly permeable to calcium, and calcium imaging data demonstrated that neurons ...
  • The N -methyl- d -aspartate (NMDA) glutamate receptor (NMDAR), long implicated in developmental plasticity, shows decay time kinetics that shorten postnatally as NR2A subunits are added to the receptor. (pnas.org)
  • In visual pathways, N -methyl- d -aspartate (NMDA) receptors (NMDARs) contain NR1 (GluR ζ1) plus varying proportions of NR2A (GluR ɛ1) and NR2B (GluR ɛ2) subunits ( 1 , 2 ). (pnas.org)
  • We report the clinical features and course of pediatric patients presenting with anti-N-methyl D-aspartate receptor (NMDA-R) encephalitis. (unboundmedicine.com)
  • TY - JOUR T1 - Pediatric anti-NMDA (N-methyl D-aspartate) receptor encephalitis. (unboundmedicine.com)
  • Anti-N-methyl-D-aspartate (NMDA)-receptor encephalitis is a serious, complex, and potentially fatal disease in children. (nih.gov)
  • 1. We have previously shown that toluene dose-dependently inhibits recombinant N-methyl-D-aspartate (NMDA) receptors at micromolar concentrations. (nih.gov)
  • 4. The convulsant solvent flurothyl had no effect on NMDA responses in oocytes but potently inhibited ion flux through recombinant GABA receptors expressed in oocytes. (nih.gov)
  • 5. Overall, these results suggest that abused solvents display pharmacological selectivity and that NR1/2B NMDA receptors may be an important target for the actions of these compounds on the brain. (nih.gov)
  • Concentration-response curves for inhibition of NMDA-induced currents by several alkylbenzenes and TCE in oocytes expressing NR1/2A or NR1/2B receptors. (nih.gov)
  • Anti- N -methyl-D-aspartate-receptor (NMDA-R) encephalitis is a new autoimmune disorder, often paraneoplastic in nature, presenting with complex neuropsychiatric symptoms. (dovepress.com)
  • 2 In slices, the potencies of the weakly (or non-) transported analogues, N-methyl-D-aspartate (NMDA) and kainate (KA) (EC 50 = 40 μM each) were higher than those of the transported amino acids, D- and L-aspartate (EC 50 = 250 μM and 300 μM) and D- and L-glutamate (EC 50 = 540 μM and 480 μM). (wiley.com)
  • Responses to NMDA, L-glutamate and L-aspartate under these conditions were equally sensitive to inhibition by APV but the response to KA remained relatively resistant to this antagonist. (wiley.com)
  • ii) the potency of APV towards the actions of transported agonists acting at NMDA receptors being reduced and (iii) a differential sensitivity to APV of responses to L-glutamate and L-aspartate being created, the consequence being that a potent action of L-glutamate on NMDA receptors is disguised. (wiley.com)
  • Comparative outcomes in children and adults with anti- N -methyl- d -aspartate (anti-NMDA) receptor encephalitis. (springer.com)
  • Guasp M, Dalmau J. Encephalitis associated with antibodies against the NMDA receptor. (springer.com)
  • Treatment and prognostic factors for long-term outcome in patients with anti-NMDA receptor encephalitis: an observational cohort study. (springer.com)
  • Schmitt SE, Pargeon K, Frechette ES, Hirsch LJ, Dalmau J, Friedman D. Extreme delta brush: a unique EEG pattern in adults with anti-NMDA receptor encephalitis. (springer.com)
  • Foff EP, Taplinger D, Suski J, Lopes MB, Quigg M. EEG findings may serve as a potential biomarker for anti-NMDA receptor encephalitis. (springer.com)
  • Hinson HE, Takahashi C, Altowaijri G, Baguley IJ, Bourdette D. Anti-NMDA receptor encephalitis with paroxysmal sympathetic hyperactivity: an under-recognized association? (springer.com)
  • Maneta E, Garcia G. Psychiatric manifestations of anti-NMDA receptor encephalitis: neurobiological underpinnings and differential diagnostic implications. (springer.com)
  • The primary aim is to determine whether perioperative NMDA-receptor antagonism has differential effects on postoperative pain, hyperalgesia and morbidity in younger and older patients. (clinicaltrials.gov)
  • In order to achieve this aim, the researchers propose to conduct the first randomized, double-blind placebo-controlled study designed to investigate age differences in the effects of perioperative oral administration of an NMDA-receptor antagonist (amantadine) in men undergoing radical prostatectomy. (clinicaltrials.gov)
  • C-fibres release glutamate which acts at three receptor types: metabotropic, kainate/AMPA and NMDA. (clinicaltrials.gov)
  • NMDA receptor activation, through a complex cascade of intracellular events, results in dorsal horn neuron hyperexcitability or central sensitization. (clinicaltrials.gov)
  • In humans, NMDA-receptor antagonism decreases secondary hyperalgesia subsequent to experimentally-induced pain. (clinicaltrials.gov)
  • However, during hypoxia, intracellular [Ca2+] increases to neurotoxic levels, mediated largely by the N-methyl-D-aspartate (NMDA) subfamily of glutamate receptors. (biologists.org)
  • Employing cell-attached single-channel patch-clamp techniques, we studied the effect of adenosine (200 micromol l-1) and anoxia on NMDA receptor open probability (Popen) and current amplitude. (biologists.org)
  • Therefore, during anoxia, NMDA receptors cannot be regulated by Mg2+ in a manner dependent on membrane potential. (biologists.org)
  • We conclude that anoxia modulates NMDA receptor activity and that adenosine plays a key role in mediating this change. (biologists.org)
  • N -methyl-D-aspartate receptor (NMDA-R) antibody encephalitis is an immune-mediated disorder characterized by the presence of anti-NMDA antibody in serum and cerebrospinal fluid, with a characteristic combination of psychological and neurological signs and symptoms. (nursingcenter.com)
  • Recent pharmacological studies have led to the hypothesis that aminoglycoside-induced ototoxicity is an excitotoxic process mediated, at least in part, by a polyamine-like modulation of N -methyl- d -aspartate (NMDA) receptors. (aspetjournals.org)
  • To explore this hypothesis, we compared the effects of several aminoglycosides (neomycin B, kanamycin A, streptomycin, and dihydrostreptomycin) with spermine on recombinant NMDA receptors of defined composition expressed in Xenopus oocytes. (aspetjournals.org)
  • No direct relationships emerged between the effect of an aminoglycoside at a specific NMDA receptor subtype and the ototoxicity of these antibiotics. (aspetjournals.org)
  • Recent pharmacological evidence suggests that aminoglycoside-induced ototoxicity is, in part, an excitotoxic process mediated by an activation of N -methyl- d -aspartate (NMDA) receptors. (aspetjournals.org)
  • Neurochemical studies indicate aminoglycosides mimic the actions of polyamines such as spermine at native NMDA receptors. (aspetjournals.org)
  • These findings led to the proposal that a polyamine-like activation of NMDA receptors is a pivotal step in the ototoxicity produced by these aminoglycosides ( Skolnick, 1997 ). (aspetjournals.org)
  • After the initial demonstration that endogenous polyamines modulate radioligand binding to NMDA receptors, electrophysiological studies in primary neuron cultures have revealed that polyamines produce multiple actions at NMDA receptors ( Benveniste and Mayer, 1993 ). (aspetjournals.org)
  • Anti- N -methyl- d -aspartate (NMDA) encephalitis is an autoimmune disorder in which antibodies are formed against NMDA receptors. (psychiatrist.com)
  • Results from the diagnostic workup revealed anti-NMDA receptor antibodies and elevated factor VIII levels. (psychiatrist.com)
  • This case illustrates the complexities associated with diagnosing and treating anti-NMDA receptor encephalitis. (psychiatrist.com)
  • N- -methyl-D-aspartate (NMDA) receptor encephalitis usually occurs in young, otherwise healthy women. (jaoa.org)
  • 1 Frequently, the diagnosis of NMDA receptor encephalitis is delayed because of the nature of the symptoms, with resulting delays in treatment and worse long-term neurologic outcomes. (jaoa.org)
  • Previous studies indicate that haloperidol, a therapeutically useful antipsychotic drug, inhibits neuronal N-methyl-D-aspartate (NMDA) responses and has neuroprotective effects against NMDA-induced brain injury. (aspetjournals.org)
  • To further characterize this inhibition, we used electrical recordings to assay the effects of haloperidol on four diheteromeric subunit combinations of cloned rat NMDA receptors expressed in Xenopus laevis oocytes: NR1A coexpressed with NR2A, NR2B, NR2C, or NR2D. (aspetjournals.org)
  • Inhibition of macroscopic neuronal NMDA responses is mechanistically similar to inhibition of NR1A/2B receptors. (aspetjournals.org)
  • Collectively, our experiments indicate that haloperidol selectively inhibits NMDA receptors comprised of NR1 and NR2B subunits. (aspetjournals.org)
  • Our results suggest that haloperidol can be used as a tool for investigating NMDA receptor subunit composition and can serve as a structural lead for designing novel subtype-selective NMDA receptor ligands. (aspetjournals.org)
  • Anti-N-methyl-D-aspartate (NMDA) receptor antibody in serum and CSF were negative. (omicsonline.org)
  • NMDA receptor antibody was strongly positive in CSF and weak positive in serum. (omicsonline.org)
  • The effects of aminoglycoside antibiotics on N- methyl- d -aspartate (NMDA) receptors were studied using voltage-clamp recording of recombinant NMDA receptors expressed in Xenopus oocytes. (aspetjournals.org)
  • We measured the effects of aminoglycosides at mutant NMDA receptors to determine which amino acid residues in NMDA receptor subunits are involved in stimulation. (aspetjournals.org)
  • Several aminoglycosides produced a weak voltage-dependent block of NMDA receptors, but the degree of inhibition did not appear to correlate with the number of amino groups in the molecule. (aspetjournals.org)
  • The results suggest that aminoglycosides having more than three amino groups have stimulatory effects that are mediated through the spermine-binding site on NMDA receptors. (aspetjournals.org)
  • Ketamine, a noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist, is frequently used in pediatric general anesthesia. (nih.gov)
  • Ketamine exposure resulted in elevated NMDA receptor (NR1) expression, increased generation of reactive oxygen species (ROS) as indicated by higher levels of 8-oxoguanine production, and enhanced neuronal damage. (nih.gov)
  • NMDA receptors regulate channels that are highly permeable to calcium, and calcium imaging data demonstrated that neurons exposed to ketamine had a significantly elevated amplitude of calcium influx and higher intracellular free calcium concentrations ([Ca(2+)]i) evoked by NMDA (50 µM), compared with control neurons. (nih.gov)
  • These findings suggest that prolonged ketamine exposure produces an increase in NMDA receptor expression (compensatory upregulation), which allows for a higher/toxic influx of calcium into neurons once ketamine is removed from the system, leading to elevated ROS generation and neuronal cell death. (nih.gov)
  • Conantokin G (Con G) is a 17-amino-acid peptide antagonist of N -methyl- d -aspartate (NMDA) receptors isolated from the venom of the marine cone snail, Conus geographus . (aspetjournals.org)
  • In this study the mechanism of action and subunit selectivity of Con G was examined in whole-cell voltage-clamp recordings from cultured neurons and in two electrode voltage-clamp recordings from Xenopus oocytes expressing recombinant NMDA receptors. (aspetjournals.org)
  • Furthermore, in oocytes expressing NR1a/NR2B receptors, Con G produced a rightward shift in the concentration-response curve for NMDA, providing support for a competitive interaction with the NMDA-binding site. (aspetjournals.org)
  • Finally, Con G selectively blocked NMDA receptors containing the NR2B subunit. (aspetjournals.org)
  • These results demonstrate that Con G is a subunit-specific competitive antagonist of NMDA receptors. (aspetjournals.org)
  • The present proposal describes the first direct comparison of perioperative NMDA receptor blockade coupled with intra- and post-operative opioid administration in young and elderly patients. (knowcancer.com)
  • NMDA receptors are among the most studied receptors in neuroscience because they are involved in neuronal cell development and plasticity, a cellular correlate for learning. (neuromics.com)
  • NMDA receptors are also implicated in several disorders of the central nervous system including epilepsy and ischemic neuronal cell death. (neuromics.com)
  • NMDA receptors also appear to be a target for ethanol at physiological concentrations and therefore may play a significant role in alcoholism. (neuromics.com)
  • Activation of the NMDA receptor or opening of the ion channel allows flow of Na+ and Ca2+ ions into the cell, and K+ out of the cell (1). (neuromics.com)
  • A gene on chromosome 17q25 that encodes an epsilon subunit of N-methyl-D-aspartate (NMDA) receptors, which belong to the glutamate receptor channel superfamily. (thefreedictionary.com)
  • NMDA receptors consist of multiple subunits arranged to form a ligand-gated ion channel, which play a key role in long-term potentiation and the plasticity of synapses (central to memory and learning). (thefreedictionary.com)
  • NMDA receptors are ligand-gated ion channels that mediate excitatory neurotransmission in the brain. (eurekamag.com)
  • Subunit-selective antagonists that discriminate between the glycine sites of GluN1 and GluN3 subunits would be valuable pharmacological tools for studies on the function and physiological roles of NMDA receptor subtypes. (eurekamag.com)
  • In addition, TK40 displayed >100-fold selectivity for GluN1/N2 NMDA receptors over GluN3A- and GluN3B-containing NMDA receptors and no appreciable effects at AMPA receptors. (eurekamag.com)
  • In rat brain cortex synaptosomes superfused with Mg 2+ -free solution containing glycine, [ 3 H]noradrenaline ( 3 H-NA) release evoked by NMD A was abolished by omission of glycine or Ca 2+ and inhibited by Mg 2+ , the competitive and noncompetitive NMDA receptor antagonists CGP 37849 and dizocilpine (MK-801), respectively, as well as by ethanol, but was not affected by tetrodotoxin. (springer.com)
  • In conclusion, presynaptic NMDA receptors mediate stimulation of NA release. (springer.com)
  • Fink K, Göthert M, Molderings G, Schlicker E (1989) N-Methyl-D-aspartate (NMDA) receptor-mediated stimulation of noradrenaline release, but not of other neurotransmitters, in the rat brain cortex: receptor location, characterization and desensitization. (springer.com)
  • Fink K, Bönisch H, Gothert M (1990) Presynaptic NMDA receptors stimulate noradrenaline release in the cerebral cortex. (springer.com)
  • Göthert M, Fink K (1989) Inhibition of N-methyl-D-aspartate ( NMDA)- and L- glutamate-induced noradrenaline and acetylcholine release in the rat brain by ethanol. (springer.com)
  • We have identified a series of positive allosteric NMDA receptor (NMDAR) modulators derived from a known class of GluN2C/D-selective tetrahydroisoquinoline analogues that includes CIQ. (figshare.com)
  • While excessive levels of glutamate result in neurotoxicity, in part through the over-activation of NMDARs, memantine-as a partial NMDAR antagonist, blocks the NMDA glutamate receptors to normalize the glutamatergic system and ameliorate cognitive and memory deficits. (eurekaselect.com)
  • David Olivares, Varun K. Deshpande, Ying Shi, Debomoy K. Lahiri, Nigel H. Greig, Jack T. Rogers and Xudong Huang, "N-Methyl D-Aspartate (NMDA) Receptor Antagonists and Memantine Treatment for Alzheimer's Disease, Vascular Dementia and Parkinson's Disease", Current Alzheimer Research (2012) 9: 746. (eurekaselect.com)
  • This released glutamate activates ionotropic glutamate receptors such as α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid and N -methyl-d-aspartate (NMDA) receptors in the postsynaptic membrane of the DH neurons, causing membrane depolarization and the firing of action potentials. (asahq.org)
  • The importance of the NMDA receptor in excitatory glutamatergic neurotransmission and in many processes such as pain sensation, 10 learning and memory, 11-13 and development 14 that are subject to plasticity makes this receptor a key player to consider in opioid tolerance. (asahq.org)
  • However, the mechanisms responsible for the NMDA receptor plasticity, particularly in response to chronic MOR activation, are unclear and understudied. (asahq.org)
  • Anti-N-methyl-D-aspartate receptor encephalitis in young healthy women while rare may be the result of an ovarian teratoma that produces anti-NMDA receptor antibodies. (uiowa.edu)
  • Patients with anti-NMDA receptor encephalitis usually have an acute onset. (biomedcentral.com)
  • Here, we describe a case of anti-NMDA receptor encephalitis with multifocal subcortical white matter lesions on fluid-attenuated inversion recovery (FLAIR) and diffuse weighted images (DWI). (biomedcentral.com)
  • Opioid tolerance can be modulated by the N-methyl- D -aspartate/nitric oxixde (NMDA/NO) cascade. (nature.com)
  • Evidence exploring a daily injection paradigm indicates that agents antagonizing NMDA receptors can prevent tolerance to morphine and delta drugs, but not kappa agents. (nature.com)
  • Even an agent acting as an antagonist on the glycine site of the NMDA receptor is effective. (nature.com)
  • Control of βAR- and N-methyl-D-aspartate (NMDA) Receptor-Dependent cAMP Dynamics in Hippocampal Neurons. (ox.ac.uk)
  • Uncompetitive N-methyl-D-aspartate (NMDA) receptor antagonists with fast off-rate (UFO) may represent promising drug candidates for various neurodegenerative disorders. (elsevier.com)
  • In this study, we report that bis(propyl)-cognitin, a novel dimeric acetylcholinesterase inhibitor and γ-aminobutyric acid subtype A receptor antagonist, is such an antagonist of NMDA receptors. (elsevier.com)
  • Molecular docking simulations showed moderate hydrophobic interaction between bis(propyl)-cognitin and the MK-801 binding region in the ion channel pore of the NMDA receptor. (elsevier.com)
  • Moreinterestingly, under NMDA receptor-mediated physiological conditions, bis(propyl)-cognitin enhanced long-term potentiation in hippocampal slices, whereas MK-801 reduced and memantine did not alter this process. (elsevier.com)
  • These results suggest that bis(propyl)-cognitin is a UFO antagonist of NMDA receptors with moderate affinity, which may provide a pathologically activated therapy for various neurodegenerative disorders associated with NMDA receptor dysregulation. (elsevier.com)
  • Subchronic treatment with memantine using osmotic pumps in male rats was used to verify whether plasma levels significantly blocking L-N-methyl-D-aspartate (NMDA) receptors (and shown previously to be neuroprotective) may impair learning. (warwick.ac.uk)
  • In-vivo NMDA receptor occupancy experiments demonstrated significant, dose-dependent receptor occupancy of 32.7 and 65.7% by memantine at the doses producing 1 and 5 μmol/l plasma levels, respectively. (warwick.ac.uk)
  • In conclusion, a dose of memantine which produces a plasma level (1 μmol/l) within the therapeutic range, reported previously to be neuroprotective, leads to intracellular brain levels similar to the affinity of memantine for NMDA receptors (receptor binding, patch clamp). (warwick.ac.uk)
  • This has been also extended by the experiments showing that at this plasma concentration, memantine occupies ca. 30% NMDA receptors in the brain and produces no cognitive impairment. (warwick.ac.uk)
  • Acute isolation of hippocampal CA3 pyramidal cells using trypsin produces neurons which respond to kainate and quisqualate but not N-methyl-d-aspartate (NMDA). (elsevier.com)
  • These data indicate that the NMDA receptor has a trypsin-sensitive component which is necessary for agonist recognition or ion channel activation. (elsevier.com)
  • The effect of extracellular and intracellular Na + on the single-channel kinetics of Mg 2+ block was studied in recombinant NR1-NR2B NMDA receptor channels. (northwestern.edu)
  • abstract = "The effect of extracellular and intracellular Na+ on the single-channel kinetics of Mg2+ block was studied in recombinant NR1-NR2B NMDA receptor channels. (northwestern.edu)
  • Clinical Features, Treatment, and Outcome of 500 Patients with Anti-NMDA Receptor Encephalitis. (pediatricneurologybriefs.com)
  • Extreme delta brush: a unique EEG pattern in adults with anti-NMDA receptor encephalitis. (pediatricneurologybriefs.com)
  • Many cases are self-limiting and respond well to IMMUNOMODULATORY THERAPIES against the NMDA RECEPTORS antibodies. (uchicago.edu)
  • Cognitive deficits following anti-NMDA receptor encephalitis. (lookformedical.com)
  • Anti-NMDA receptor encephalitis: an important differential diagnosis in psychosis. (lookformedical.com)
  • Anti-NMDA receptor encephalitis presenting with focal non-convulsive status epilepticus in a child. (lookformedical.com)
  • Anti-NMDA-receptor antibody detected in encephalitis, schizophrenia, and narcolepsy with psychotic features. (lookformedical.com)
  • s can cause an autoimmune illness called Anti N- methyl -D- aspartate (NMDA) receptor encephalitis . (lookformedical.com)
  • Anti -NMDA receptor encephalitis ", was identified as a serious complication. (lookformedical.com)
  • N-methyl- D-aspartate (NMDA) receptors are involved in the development of central sensitization associated with chronic refractory pain syndromes. (painmanagementcenterinc.com)
  • 4-Benzylpiperidine-1-yl)-(6-hydroxy-1H-indole-2-yl)-methanone (6a) derived from (E)-1 -(4-benzylpiperidin-1-yl)-3-(4-hydroxy-phenyl)-propenone (5) was identified as a potent NR2B subunit-selective antagonist of the NMDA receptor. (elsevier.com)
  • The present study was aimed to investigate effect of sulfite on the N-methyl-D-aspartate (NMDA) receptor (NMDAR) NR2A and NR2B subunits in hippocampus of normal and SOX-deficient rats. (mysciencework.com)
  • These cognitive and behavioral effects are dose-dependently induced by ketamine and other antagonists of the N-methyl-D-aspartate (NMDA) glutamate receptor. (clinicaltrials.gov)
  • NMDA receptor hypofunction can disinhibit excitatory (cholinergic/glutamatergic) projections in key areas of the brain, and this has been proposed to explain key features of schizophrenia. (clinicaltrials.gov)
  • Several treatments that block excessive excitatory transmitter release have also been shown to prevent cognitive and behavioral effects of ketamine-induced NMDA receptor hypofunction in humans. (clinicaltrials.gov)
  • Graphs represent the average timecourse of N -methyl- d -aspartate receptor component of field excitatory postsynaptic potentials (NMDA-fEPSPs). (biomedcentral.com)
  • The N-methyl-D-aspartate (NMDA) receptor NR1 gene encodes RNA that is alternatively spliced to generate at least seven variants. (elsevier.com)
  • NR1 receptors that lacked the N-terminal exon (NR1 000 , NR1 010 , and NR1 011 ) exhibited a relatively high affinity for NMDA (EC 50 ≈ 13 μM) and marked potentiation by spermine. (elsevier.com)
  • These findings identify the contributions of the separate polypeptide domains to modulation by polyamines and PKC and provide further support for the concept that subunit composition determines functional properties of NMDA receptors. (elsevier.com)
  • The stimulatory influence of N-methyl-D-aspartate (NMDA), a glutamate receptor agonist, on LH secretion is well established in several mammalian species including the rhesus macaque. (elsevier.com)
  • A second experiment examined whether prazosin, an α-adrenergic receptor antagonist, could attenuate NMDA-induced stimulation of LH release. (elsevier.com)
  • Therefore, in spite of the evidence that at least some of the noradrenergic neurons of the primate hindbrain express the NMDAR1 receptor subunit, it is unlikely that noradrenergic inter-neuronal pathways alone play a major role in mediating the stimulators action of NMDA on GnRH/LH secretion in primates. (elsevier.com)
  • Hess, David L. / α-Adrenergic receptor antagonism and N-methyl-D-aspartate (NMDA) induced luteinizing hormone release in female rhesus macaques . (elsevier.com)
  • Points represent mean ± SEM of the N -methyl- d -aspartate receptor component of field excitatory postsynaptic potential (NMDA-fEPSP) slopes. (biomedcentral.com)
  • Glutamate Receptor Ionotropic NMDA 2B (Glutamate [NMDA] Receptor Subunit Epsilon 2 or N Methyl D Aspartate Receptor Subtype 2B or N Methyl D Aspartate Receptor Subunit 3 or GRIN2B) pipeline Target constitutes close to 11 molecules. (jsbmarketresearch.com)
  • The latest report Glutamate Receptor Ionotropic NMDA 2B - Pipeline Review, H2 2017, outlays comprehensive information on the Glutamate Receptor Ionotropic NMDA 2B (Glutamate [NMDA] Receptor Subunit Epsilon 2 or N Methyl D Aspartate Receptor Subtype 2B or N Methyl D Aspartate Receptor Subunit 3 or GRIN2B) targeted therapeutics, complete with analysis by indications, stage of development, mechanism of action (MoA), route of administration (RoA) and molecule type. (jsbmarketresearch.com)
  • Glutamate Receptor Ionotropic NMDA 2B (Glutamate [NMDA] Receptor Subunit Epsilon 2 or N Methyl D Aspartate Receptor Subtype 2B or N Methyl D Aspartate Receptor Subunit 3 or GRIN2B) - Glutamate receptor subunit epsilon-2 or N-methyl D-aspartate receptor subtype 2B (NMDAR2B or NR2B) is a protein encoded by the GRIN2B gene. (jsbmarketresearch.com)
  • Its phosphorylation at Ser-1303 by DAPK1 enhances synaptic NMDA receptor channel activity inducing injurious Ca2+ influx through them resulting in an irreversible neuronal death. (jsbmarketresearch.com)
  • Furthermore, this report also reviews key players involved in Glutamate Receptor Ionotropic NMDA 2B (Glutamate [NMDA] Receptor Subunit Epsilon 2 or N Methyl D Aspartate Receptor Subtype 2B or N Methyl D Aspartate Receptor Subunit 3 or GRIN2B) targeted therapeutics development with respective active and dormant or discontinued projects. (jsbmarketresearch.com)
  • Glutamate excitotoxicity to a large extent is mediated through activation of the N -methyl- d -aspartate (NMDA)-gated ion channels in several neurodegenerative diseases and ischemic stroke. (jimmunol.org)
  • Activation of the N -methyl- d -aspartate (NMDA) 3 receptors to a large extent mediates the glutamate excitotoxicity and neuronal death in several neurodegenerative diseases and ischemic stroke ( 1 , 2 , 3 ). (jimmunol.org)
  • Subsequent to activation of NMDA receptors occurs toxic calcium influx, which activates numerous enzymes, including neuronal NO synthase (NOS). (jimmunol.org)
  • Importantly, several studies have shown that the neurotoxicity of microglial toxins is mediated through the NMDA receptor (NMDAR), involving either glutamate and quinolinic acid or a still uncharacterized NMDAR binding molecule ( 18 , 19 , 20 , 21 ). (jimmunol.org)
  • IMSEAR at SEARO: N-methyl-D-aspartate (NMDA) receptor: friend or foe? (who.int)
  • What is the role of ethanol and N-methyl-D-aspartate (NMDA) in the pathogenesis of delirium tremens (DTs)? (medscape.com)
  • Ethanol also acts as an NMDA receptor antagonist. (medscape.com)
  • The clinical manifestations of ethanol withdrawal are due to the combination of effects on the GABA and NMDA receptors. (medscape.com)
  • Studies have shown that N-methyl-d-aspartate (NMDA) receptors are among the ligand-gated ion channels affected by prenatal ethanol exposure. (unm.edu)
  • Primary cultures of hippocampal neurons were prepared from the neonatal offspring of these dams, and NMDA receptor function was assessed by patch clamp electrophysiological techniques after 6-7 days in culture in ethanol-free media. (unm.edu)
  • Unexpectedly, we did not detect any changes in hippocampal NMDA receptor function at either the whole-cell or single-channel levels. (unm.edu)
  • However, we determined that fetal alcohol exposure alters the actions of the neurosteroids pregnenolone sulfate and pregnenolone hemisuccinate, which potentiate NMDA receptor function. (unm.edu)
  • Western immunoblot analyses demonstrated that this alteration is not due to a change in the expression levels of NMDA receptor subunits. (unm.edu)
  • Importantly, in utero ethanol exposure did not affect the actions of neurosteroids that inhibit NMDA receptor function. (unm.edu)
  • Moreover, the actions of pregnenolone sulfate on type A gamma-aminobutyric acid and non-NMDA receptor function were unaltered by ethanol exposure in utero, which suggests that the alteration is specific to NMDA receptors. (unm.edu)
  • Felbamate has been proposed to have a unique dual mechanism of action as a positive modulator of GABAA receptors and as a blocker of NMDA receptors, particularly isoforms containing the NR2B subunit. (wikipedia.org)
  • Although it is clear that felbamate does cause pharmacological inhibition of NMDA receptors, the relevance of NMDA receptor blockade as a strategy for the treatment of human epilepsy has been questioned. (wikipedia.org)
  • Therefore, the importance of the effects of felbamate on NMDA receptors to its therapeutic action in epilepsy is uncertain. (wikipedia.org)
  • Using this system, she and her colleagues demonstrated the importance of NMDA receptors in development plasticity. (wikipedia.org)
  • The rehabilitation of children with anti-N-methyl-D-aspartate-receptor encephalitis: a case series. (nih.gov)
  • In this case series, we report on six known consecutive pediatric cases of N-methyl-D-aspartate-receptor antibody encephalitis in Northern California requiring comprehensive inpatient rehabilitation. (nih.gov)
  • Because of the complicated management and extensive rehabilitation needs of children with anti-N-methyl-D-aspartate-receptor encephalitis, physiatrists and other rehabilitation providers should be knowledgeable about this complex condition. (nih.gov)
  • Anti-N-methyl-D-aspartate receptor (anti-NMDAR) encephalitis is a treatment-responsive encephalitis associated with anti-NMDAR antibodies. (unboundmedicine.com)
  • Patients with N -methyl- d -aspartate receptor encephalitis (NMDARE) usually present with amnesia, seizures, psychiatric symptoms, dyskinesias, and autonomic dysfunction. (springer.com)
  • Anti- N -methyl-d-aspartate receptor (NMDAR) encephalitis is a form of autoimmune encephalitis associated with antibodies against the NR1 subunits of NMDARs. (dovepress.com)
  • Anti-N-methyl-D-aspartate receptor (NMDAR) encephalitis is a recently discovered autoimmune syndrome associated with psychosis, dyskinesias, and seizures. (mdc-berlin.de)
  • Malayev Y, Alberts J, Verardi MA, Mattison AR, Imlay S. Immature Teratoma Associated With Anti- N -Methyl-D-Aspartate Receptor Encephalitis. (jaoa.org)
  • Anti- N -methyl-D-aspartate receptor encephalitis was diagnosed and, with excision and medical management, her symptoms resolved and she was discharged home in stable condition. (jaoa.org)
  • Encephalopathy is not commonly attributed to gynecologic causes, but anti- N -methyl-D-aspartate receptor encephalitis may be caused by ovarian teratomas with a neuronal component. (jaoa.org)
  • In recent years, more and more medical researchers realized that anti-N-methyl-D-aspartate receptor (NMDAR) encephalitis can be triggered by herpes simplex encephalitis (HSE), which can lead to an immune-mediated relapse. (omicsonline.org)
  • Anti-N-Methyl-D-Aspartate receptor encephalitis is a type of in lammation of brain which can be lethal if remains untreated. (omicsonline.org)
  • Here we report a case of a 20-year-old Chinese male student where anti-N-methyl-D-aspartate receptor (NMDAR) encephalitis as triggered by herpes simplex encephalitis. (omicsonline.org)
  • Anti- N -methyl-D-aspertate receptor encephalitis is an autoimmune-mediated disease without specific brain MRI features. (ajnr.org)
  • Our aim was to investigate the brain MR imaging characteristics of anti- N -methyl-D-aspartate receptor encephalitis and their associations with clinical outcome at a 2-year follow-up. (ajnr.org)
  • We enrolled 53 patients with anti- N -methyl-D-aspartate receptor encephalitis and performed 2-year follow-up. (ajnr.org)
  • N-methyl-D-aspartate receptor antibodies should be tested in patients with hyperkinetic encephalitis and neuropsychiatric prodrome admitted to the intensive care unit. (ovid.com)
  • Objective N-methyl-D-aspartate receptor antibody (NMDAR-Ab) encephalitis is a well-recognised clinico-immunological syndrome that presents with neuropsychiatric symptoms cognitive decline, movement disorder and seizures. (bmj.com)
  • Anti-N-methyl-D-aspartate receptor (anti-NMDAR) encephalitis is a well-recognised disorder, first fully characterised in 2007. (bmj.com)
  • Anti-N-methyl-D-aspartate receptor encephalitis and teratoma" by Colette M. Gnade, Heather R. Williams et al. (uiowa.edu)
  • This includes an evaluation for anti-N-methyl-D-aspartate receptor encephalitis. (uiowa.edu)
  • Anti-N-methyl-D-aspartate receptor encephalitis is a severe autoimmune disorder characterized by severe psychiatric symptoms, seizures, decreased consciousness, autonomic dysregulation, and dyskinesias. (biomedcentral.com)
  • Identification of anti-N-methyl-D-aspartate receptor antibodies in serum and cerebrospinal fluid confirmed the diagnosis of anti-N-methyl-D-aspartate receptor encephalitis. (biomedcentral.com)
  • Anti-N-methyl-D-aspartate receptor encephalitis may be concomitant with multifocal subcortical white matter lesions. (biomedcentral.com)
  • Aim: To determine the validity of the proposed clinical diagnostic criteria for anti‐N‐methyl‐d‐aspartate receptor (NMDAR) encephalitis in paediatric patients. (ucl.ac.uk)
  • What this paper adds: The proposed clinical diagnostic criteria for anti‐N‐methyl‐d‐aspartate receptor (NMDAR) encephalitis by Graus et al. (ucl.ac.uk)
  • Anti-N-Methyl-D-Aspartate Receptor Encephalitis: A Review of Psychiatric Phenotypes and Management Considerations. (ox.ac.uk)
  • Anti-N-Methyl-D-Aspartate Receptor Encephalitis In A Young Child With Histological Evidence On Brain Biopsy Of Coexistent Herpes Simplex Virus Type 1 Infection. (ox.ac.uk)
  • We report a 3-year-old boy with anti-N-methyl-D-aspartate receptor encephalitis with a typical syndrome of movement disorder and encephalopathy and evidence of herpes simplex virus (HSV) type 1 infection on brain biopsy. (ox.ac.uk)
  • HSV type 1 infection and anti-N-methyl-D-aspartate receptor encephalitis are temporally linked in some cases: this case suggests that prodromal HSV type-1 infection may be clinically subtle and easily missed. (ox.ac.uk)
  • Abstract Anti-N-methyl-D-aspartate receptor (anti-NMDAR) encephalitis is a relatively new autoimmune disorder of the central nervous system. (openaire.eu)
  • In N-methyl-D-aspartate encephalitis it is well recognized that a tumor (mainly an ovarian teratoma) or a herpetic infection can precede the onset of the disease, but in the majority of cases the trigger remains unknown. (springer.com)
  • Investigators at Universities of Barcelona, Pennsylvania, Oviedo, and Valencia, and the Spanish NMDAR Encephalitis Work Group report the clinical features of 20 pediatric patients with anti-N-methyl-D-aspartate receptor (NMDAR) encephalitis seen in a single center in Spain in the last 4 years. (pediatricneurologybriefs.com)
  • 2013). Pediatric anti-N-methyl-D-aspartate receptor encephalitis - Clinical analysis and novel findings in a series of 20 patients. (pediatricneurologybriefs.com)
  • 2009). Anti-N-methyl-D-aspartate receptor (NMDAR) encephalitis in children and adolescents. (pediatricneurologybriefs.com)
  • Anti-N-Methyl-D-Aspartate Receptor Encephalitis" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (uchicago.edu)
  • This graph shows the total number of publications written about "Anti-N-Methyl-D-Aspartate Receptor Encephalitis" by people in this website by year, and whether "Anti-N-Methyl-D-Aspartate Receptor Encephalitis" was a major or minor topic of these publications. (uchicago.edu)
  • Below are the most recent publications written about "Anti-N-Methyl-D-Aspartate Receptor Encephalitis" by people in Profiles. (uchicago.edu)
  • Safety of Electroconvulsive Therapy in 2 Very Young Pediatric Patients With Catatonia Related to Anti-N-methyl-D-aspartate Receptor Encephalitis. (uchicago.edu)
  • Anti-N-methyl-D-aspartate receptor encephalitis: an emerging cause of centrally mediated sinus node dysfunction. (lookformedical.com)
  • Fluorodeoxyglucose positron emission tomography in anti-N-methyl-D-aspartate receptor encephalitis: distinct pattern of disease. (lookformedical.com)
  • Anti-N-methyl-D-aspartate receptor (NMDAR) encephalitis has been increasingly recognized in recent years. (nnjournal.net)
  • Anti-N-methyl-D-aspartate-receptor encephalitis: cognitive profile in two children. (ox.ac.uk)
  • BACKGROUND: Anti-N-Methyl D-aspartate receptor (NMDAR) encephalitis is an autoimmune disorder associated with antibodies against NMDAR resulting in a characteristic neuropsychiatric syndrome characterized by seizures, dyskinesias, and cognitive impairment. (ox.ac.uk)
  • N-methyl-D-aspartate receptor (NMDAR) forms a heterodimer of at least one NR1 and one NR2A-D subunit. (neuromics.com)
  • We have proposed that tPA potentiates excitotoxicity by interacting with and cleaving the aminoterminal end of the NR1 subunit of N -methyl- d -aspartate receptors, leading to an increased calcium influx, Erk1/2 activation, and neurotoxicity. (ahajournals.org)
  • Conclusion- We demonstrate that the tPA-dependent interaction and cleavage of the NR1 subunit of N -methyl- d -aspartate receptors occurs in vivo after stroke and that this interaction is a relevant therapeutic target for stroke treatment. (ahajournals.org)
  • To elucidate whether a permanent reduction of the GluN2B subunit affects the pathology of Alzheimer's disease (AD), we cross-bred mice heterozygous for GluN2B receptors in the forebrain (hetGluN2B) with a mouse model for AD carrying a mutated amyloid precursor protein with the Swedish and Arctic mutation (mAPP) resulting in a hetGluN2B/mAPP transgenic. (ovid.com)
  • PKC can phosphorylate the NR1 subunit (NMDAR1) of the receptor on Ser890/Ser896, and PKA can phosphorylate NR1 on Ser897 (3). (neuromics.com)
  • Characterization of nociceptin/orphanin FQ-induced pain responses in conscious mice: neonatal capsaicin treatment and N-methyl-D-aspartate receptor GluRepsilon subunit knockout mice. (curehunter.com)
  • the former is mediated by substance P and the latter is mediated by glutamate through the N-methyl-D-aspartate receptor comprising the GluRvarepsilon1 subunit. (curehunter.com)
  • Impaired social behaviors and minimized oxytocin signaling of the adult mice deficient in the N-methyl-d-aspartate receptor GluN3A subunit. (autismcandles.com)
  • α6 subunit-containing nicotinic receptors mediate low-dose ethanol effects on ventral tegmental area neurons and ethanol reward. (semanticscholar.org)
  • Nicotine exposure reduces N-methyl-D-aspartate toxicity in the hippocampus: relation to distribution of the alpha7 nicotinic acetylcholine receptor subunit. (semanticscholar.org)
  • Our previous results showed that reduction in expression of N-methyl-D-aspartate receptor 1 (NR1), the key subunit of N-methyl-D-aspartate receptors, by antisense oligos ameliorated the motor symptoms in the 6-hydroxydopamine (6-OHDA)-lesioned rat, an animal model of Parkinson's disease (PD) [Lai et al. (hku.hk)
  • Expressions of N-methyl-D-aspartate receptors NR2A and NR2B subunit proteins in normal and sulfite-oxidase deficient rat's hippocampus: effect of exogenous sulfite ingestion. (mysciencework.com)
  • In situ hybridization histochemistry, using a cRNA probe coding for the NMDAR1 receptor subunit, revealed abundant mRNA in the locus coeruleus, a brain area rich in noradrenergic neurons. (elsevier.com)
  • Furthermore, using double-label fluorescence immunocytochemistry, the tyrosine hydroxylase immunopositive neurons of the locus coeruleus showed immunoreactivity for the NMDAR1 receptor subunit protein. (elsevier.com)
  • The recent discovery of glycine transporters in both the central nervous system and the periphery suggests that glycine transport may be critical to N -methyl- d -aspartate receptor (NMDAR) function by controlling glycine concentration at the NMDAR modulatory glycine site. (pnas.org)
  • N -methyl- d -aspartate receptors (NMDAR) play a crucial role in several aspects of fast excitatory neurotransmission including the gating of an excitatory conductance with partial permeability to calcium ( 1 ) and, in some regions, long-term synaptic plasticity ( 2 ). (pnas.org)
  • Blockade was restricted to glutamate receptors in the eyecup, because only the sSC contralateral to the eye containing α-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid receptor (AMPAR) and NMDAR antagonists failed to up-regulate PSD-95 and NR2A (Fig. 5 D ). (pnas.org)
  • Since the discovery that a single dose of ketamine, an N-methyl-D-aspartate receptor (NMDAR) antagonist, had rapid and long-lasting antidepressant effects, there has been increased interest in using NMDAR modulators in the pharmacotherapy of depression. (frontiersin.org)
  • However, recent attention has focused on the NMDAR as a therapeutic target for major depression, and despite often ambiguous mechanistic insight, both inhibition and stimulation of this receptor convey antidepressant properties. (frontiersin.org)
  • This review article will critically evaluate the current literature reporting the validity of NMDAR modulation in major depression, and will propose a mechanism by which the function of this receptor in an "on" or "off" state may have antidepressant actions. (frontiersin.org)
  • N-Methyl D-aspartate receptors (NMDAR) are ligand-gated ion channels involved in numerous neurological functions, including memory, learning, and synaptic plasticity. (frontiersin.org)
  • Our functional data using primary hippocampal neurons indicate that human cerebrospinal fluid-derived monoclonal NR1 antibodies alone are sufficient to cause neuronal surface receptor downregulation and subsequent impairment of NMDAR-mediated currents, thus providing ultimate proof of antibody pathogenicity. (mdc-berlin.de)
  • Objectives We explored the impact of circulating anti-N-methyl-D-aspartate receptor (NMDAR) antibodies on the severity of fatigue in patients with systemic lupus erythematosus (SLE). (bmj.com)
  • Indeed, the interaction between tPA and the low-density lipoprotein receptor-related protein, the N-methyl- d -aspartate receptor (NMDAR), annexin II in glial cells, and/or neurons activates cell signaling processes that result in different outcomes depending on the physiological or pathological contexts. (ahajournals.org)
  • The presence of N-methyl-d-aspartate receptor (NMDAR) was previously shown in rat red blood cells (RBCs) and in a UT-7/Epo human myeloid cell line differentiating into erythroid lineage. (uzh.ch)
  • Memantine, a partial antagonist of N-methyl-D-aspartate receptor (NMDAR), approved for moderate to severe Alzheimer's disease (AD) treatment within the US and Europe under brand name Namenda (Forest), Axura and Akatinol (Merz), and Ebixa and Abixa (Lundbeck), may have potential in alleviating additional neurological conditions, such as vascular dementia (VD) and Parkinson's disease (PD). (eurekaselect.com)
  • The key to memantine's therapeutic action lies in its uncompetitive binding to the NMDAR through which low affinity and rapid off-rate kinetics of memantine at the level of the NMDAR-channel preserves the physiological function of the receptor, underpinning memantine's tolerability and low adverse event profile. (eurekaselect.com)
  • Objective N-methyl-D-aspartate receptor (NMDAR) activation and downstream transduction pathways are crucial for pain signalling. (bmj.com)
  • N-methyl-D-aspartate receptors (NMDAR) act as tumor suppressors of digestive malignancies. (biomedcentral.com)
  • The N-methyl-d-aspartate receptor (NMDAR) has been implicated in the pathophysiology of neurological diseases, such as schizophrenia, autism spectrum disorders (ASD), and Alzheimer's disease (AD), whose unique clinical hallmark is a constellation of impaired social and/or cognitive behaviors. (autismcandles.com)
  • Here we show that SLE patients carrying antibodies that bind DNA and the GluN2A and GluN2B subunits of the N-methyl-d-aspartate receptor (NMDAR), termed DNRAbs, displayed a selective impairment in spatial recall. (ntu.edu.sg)
  • Circulating autoantibodies against glutamatergic N-methyl-D-aspartate receptor (NMDAR) have been reported in a proportion of patients with psychotic disorders, raising hopes for more appropriate treatment for these antibody-positive patients. (ox.ac.uk)
  • The N-methyl-D-aspartate receptors (NMDAR) are glutamatergic ion channels that are widely expressed in both cortical and subcortical areas of the brain. (nnjournal.net)
  • Background Ketamine and non-ketamine N-methyl-d-aspartate receptor antagonists (NMDAR antagonists) recently demonstrated antidepressant efficacy for the treatment of refractory depression, but effect sizes, trajectories and possible class effects are unclear. (elsevier.com)
  • In particular, prolonged inhibition of Ca 2+ influx through N -Methyl-D-aspartate receptors (NMDAR) but not L-type voltage-gated Ca 2+ channels (VGCC) has been shown to mimic the elevation in firing frequency driven by chronic activity blockade [ 2 ]. (biomedcentral.com)
  • Multiple receptor isoforms with distinct brain distributions and functional properties arise by selective splicing of the NR1 transcripts and differential expression of the NR2 subunits. (neuromics.com)
  • The receptor tetramers in erythroid precursor cells are composed of the NR1, NR2A, 2C, 2D, NR3A, and 3B subunits of which the glycine-binding NR3A and 3B and glutamate-binding NR2C and 2D subunits prevailed. (uzh.ch)
  • Whereas this treatment markedly reduced the content of substance P in the spinal cord, it did not affect the nociceptin content or the expression of nociceptin receptors and GluRvarepsilon and GluRzeta subunits of N-methyl-D-aspartate receptors in it. (curehunter.com)
  • RESULTS: Systemically injected fusion peptide Tat-PSD-95 PDZ2 was delivered into the central nervous system, disrupted the protein-protein interactions between N-methyl-d-aspartate receptor NR2 subunits and PSD-95, and significantly reduced the minimum alveolar anesthetic concentration and righting reflex EC50 for halothane. (elsevier.com)
  • Tissues were dissected for RNA / DNA extraction and N-methyl-D-aspartate receptor subunits were analyzed using quantitative reverse transcription (RT)- PCR , ELISA and pyrosequencing . (bvsalud.org)
  • We identified N-methyl-D-aspartate receptor antibodies in six patients (two male and four female). (ovid.com)
  • N-methyl-D-aspartate receptor antibodies were identified in serum samples by an immunofluorescent cell-based assay. (ovid.com)
  • IgG).12 The naive antibody repertoire present in humans is derived from a large pool of B cells expressing diverse B-cell receptors (BCRs) generated by approximately 500 different germ line genes encoding the VL/VH, diversity, and joining segments that also hold the potential of generating thousands of antibodies of various classes (e.g. (welbourneprimary.com)
  • The Abs are directed against membrane receptors and ion channel-associated proteins that are expressed on the surface of neurons in the CNS, such as N -methyl D-aspartate receptors and leucine-rich, glioma inactivated 1 protein and contactin-associated protein like 2, that are associated with voltage-gated potassium channels. (springer.com)
  • Age-matched WT cells showed NR2A-rich receptors predominating in minis, yet slow NR2B mediated currents persisted in evoked currents. (pnas.org)
  • A number of aminoglycosides were found to potentiate macroscopic currents at heteromeric NR1 a /NR2B receptors, but not at NR1 a /NR2A, NR1 a /NR2C, NR1 a /NR2D, or NR1 b /NR2B receptors. (aspetjournals.org)
  • Expression levels of phosphorylated N-methyl-D-aspartate receptor (pNR)1 and pNR2B were significantly increased in the dorsal root ganglion of FM model mice (132.21±14.4% and 116.69±3.22% of control values), whereas NR1 and NR2B levels were unchanged (97.31±3.79% and 97.07%±2.27%, respectively). (bmj.com)
  • In the present study, N-methyl-D-aspartate receptor 2B (NR2B)-specific siRNA was applied in parkinsonian models. (hku.hk)
  • Expressions of N-methyl-D-aspartate receptors NR2A and NR2B su. (mysciencework.com)
  • Mohammed Naeem, Hala Al Alem, Ali Al Shehri, and Majed Al-Jeraisy, "Effect of N-Methyl-D-Aspartate Receptor Antagonist Dextromethorphan on Opioid Analgesia in Pediatric Intensive Care Unit," Pain Research and Management , vol. 2016, Article ID 1658172, 7 pages, 2016. (hindawi.com)
  • Receptor activity was monitored using a radiolabeled antagonist binding assay, live imaging of Ca(2+) uptake, patch clamp, and monitoring of cell volume changes. (uzh.ch)
  • Here, we show by Schild analysis that TK40 is a potent competitive antagonist with Kb values of 21-63 nM at the GluN1 glycine-binding site of the four recombinant GluN1/N2A-D receptors. (eurekamag.com)
  • GV196771 [ E -4,6-dichloro-3-(2-oxo-1-phenyl-pyrrolidin-3-glydenemethyl)-1 H -indole-2 carboxylic acid] is a potent antagonist of the modulatory glycine site of the N -methyl- d -aspartate receptor. (aspetjournals.org)
  • Methadone has the property of both m opioid receptor agonist and MNDA antagonist. (painmanagementcenterinc.com)
  • N-methyl-D-aspartate receptor antagonist desegregates eye-specific stripes. (wikipedia.org)
  • Background]: Noncompetitive N-methyl-D-aspartate receptor antagonists are widely used as pharmacological models of schizophrenia. (csic.es)
  • Lodge D, Johnson KM (1990) Noncompetitive excitatory amino acid receptor antagonists. (springer.com)
  • Watkins JC, Krogsgaard-Larsen P, Honoré T (1990) Structure-activity relationship in the development of excitatory amino acid receptor agonists and competitive antagonists. (springer.com)
  • Göthert M, Thielecke G (1976) Inhibition by ethanol of noradrenaline output from peripheral sympathetic nerves: possible interaction of ethanol with neuronal receptors. (springer.com)
  • 4-6 Prolonged MOR activation results in desensitization of the receptors through G-protein uncoupling and subsequent neuronal excitation. (asahq.org)
  • Subtype-selective inhibition of N-methyl-D-aspartate receptors by haloperidol. (aspetjournals.org)
  • Fink K, Göthert M (1990) Inhibition of N-methyl-D-aspartate-induced noradrenaline release by alcohols is related to their hydrophobicity. (springer.com)
  • Ethanol inhibition of N-methyl-D-aspartate responses involves presynaptic gamma-aminobutyric acid(B) receptors. (semanticscholar.org)
  • Importantly, inhibition of N -Methyl-D-Aspartate receptors alone mimics the effects of tetrodotoxin, including the elevation in firing frequency and reduction of potassium channel gene expression and current driven by activity blockade, whereas inhibition of L-type voltage-gated calcium channels has no effect. (biomedcentral.com)
  • D-serine, the D-stereoisomer of serine, synthesized in the brain by serine racemase from its L-stereoisomer is considered a co-agonist I co-activator of glutamatergic N-methyl-0-aspartate receptors (NMDARs). (fsu.edu)
  • Blockade of neurotensin (NT) receptors with SR-48692 prevents the development of sensitization to the locomotor activating effects of amphetamine (AMPH). (concordia.ca)
  • Collectively, our data suggest that homeostatic intrinsic plasticity induced by chronic activity blockade is accomplished in part by decreased calcium influx through N -Methyl-D-Aspartate receptors and subsequent transcriptional down-regulation of potassium channel genes. (biomedcentral.com)
  • Effects of volatile solvents on recombinant N-methyl-D-aspartate receptors expressed in Xenopus oocytes. (nih.gov)
  • We report here electrophysiological characterization of six splice variants of the NR1 receptor expressed in Xenopus oocytes. (elsevier.com)
  • The NR1/2B combination was the most sensitive receptor subtype tested with an IC(50) value for toluene of 0.17 mM. 2. (nih.gov)
  • The NR1/2B receptor subtype was several times more sensitive to these compounds than the NR1/2A subtype. (nih.gov)
  • ONE subtype of ionotropic glutamate receptors, N -methyl-d-aspartate receptors (NMDARs), is broadly distributed in the central nervous system. (asahq.org)
  • Morphine, at clinically relevant concentrations, binds primarily to the μ subtype of G i /G o protein-coupled opioid receptors, which regulate adenylyl cyclase, Ca 2+ , and K + channels. (asahq.org)
  • Of the five dopamine receptor subtypes, the D2 receptor subtype (DRD2) has been extensively studied in alcoholism [ 13 - 23 ]. (mdpi.com)
  • Like spermine, aminoglycosides potentiate agonist-induced responses in the presence of both saturating glycine ("glycine-independent") and subsaturating glycine ("glycine-dependent") concentrations on NR1A/2B receptors. (aspetjournals.org)
  • Likewise, aminoglycosides and spermine potentiated the agonist responses under glycine-dependent conditions on NR1A/2A receptors. (aspetjournals.org)
  • Inhibition of NR1A/2B receptors is insurmountable with respect to glutamate and glycine and does not exhibit voltage dependence. (aspetjournals.org)
  • In circulating RBCs the receptor activity is controlled by plasma glutamate and glycine. (uzh.ch)
  • Keith RA, Mangano TJ, Meiners BA, Stumpo RJ, Klika AB, Patel J, Salama AI (1989) HA-966 acts at a modulatory glycine site to inhibit N-methyl-D-aspartate- evoked neurotransmitter release. (springer.com)
  • In contrast, those receptor variants with the N-terminal insert (NR1 100 , NR1 101 , and NR1 111 ) showed a lower agonist affinity and little or no spermine potentiation at saturating glycine. (elsevier.com)
  • N-methyl-D-aspartate receptors (NMDARs) are known for their role in the induction of long-term potentiation (LTP). (nih.gov)
  • The N-methyl-D-aspartate receptors (NMDARs) are a class of ionotropic glutamate receptors that are widely expressed in the brain. (frontiersin.org)
  • 3. D-serine's antagonism of GluN3-containing triheteromeric NMDARs may be important because these receptors appear significantly more permeable 1 selective for calcium, a potent excitotoxicant that underlies cell death under a number of scenarios including epilepsy. (fsu.edu)
  • 15 Therefore, serine phosphorylation represents a major posttranslational modification for NMDARs in their fundamental regulation of the receptor function. (asahq.org)
  • Several forms of long-term potentiation (LTP) at the Schaffer collateral CA1 synapse require stimulation of both βARs and N-methyl-D-aspartate receptors (NMDARs). (ox.ac.uk)
  • Nicotinic receptors differentially regulate N-methyl-D-aspartate damage in acute hippocampal slices. (semanticscholar.org)
  • Fetal alcohol exposure alters neurosteroid modulation of hippocampal N-methyl-D-aspartate receptors. (unm.edu)
  • Concentration-response curves for the effects of flurothyl on oocytes expressing either NR1/2A, NR1/2B or GABA A α 1 /β 1 /γ 2s receptors. (nih.gov)
  • In oocytes from some frogs, 30-100 microM haloperidol induces potentiation of NR1A/2A receptor responses. (aspetjournals.org)
  • Cell- and Single Molecule-Based Methods to Detect Anti-N-Methyl-D-Aspartate Receptor Autoantibodies in Patients With First-Episode Psychosis From the OPTiMiSE Project. (ox.ac.uk)
  • N-Methyl-D-Aspartate Receptor Autoantibodies in Psychiatric Illness. (nihr.ac.uk)
  • Fingerprint Dive into the research topics of 'Splice variants of the N-methyl-D-aspartate receptor NR1 identify domains involved in regulation by polyamines and protein kinase C'. Together they form a unique fingerprint. (elsevier.com)
  • BACKGROUND: The authors' previous studies have shown that clinically relevant concentrations of inhalational anesthetics dose-dependently and specifically inhibit the PSD-95, Dlg, and ZO-1 (PDZ) domain-mediated protein interactions between postsynaptic density protein 95 (PSD-95) and N-methyl-d-aspartate receptors, and that the knockdown of spinal PSD-95 by intrathecal injection of PSD-95 antisense oligodeoxynucleotide significantly reduces the minimum alveolar anesthetic concentration for isoflurane in rats. (elsevier.com)
  • methyl-D-aspartate receptor changes in the brain of isolated reared rats. (bvsalud.org)
  • Norepinephrine, a neuromodulator that activates β-adrenergic receptors (βARs), facilitates learning and memory as well as the induction of synaptic plasticity in the hippocampus. (ox.ac.uk)
  • This suggests that signaling by β-adrenergic receptors depends on temporal pattern of stimulation, and that switching may represent a novel mechanism for recruiting kinases involved in synaptic plasticity and memory. (ox.ac.uk)
  • The phosphorylation of NR1 by PKA probably counteracts the inhibitory effect of calcineurin on the receptor (5). (neuromics.com)
  • 16,17 As a negative regulator of protein phosphorylation, PP2A plays a key role in the dephosphorylation of various phosphoproteins (receptors, enzymes, structural proteins, and others) in relation to many fundamental cellular activities. (asahq.org)
  • The role of specific nicotinic acetylcholine receptors (nAChRs) subtypes in mediating this effect is not well understood, however. (semanticscholar.org)
  • in contrast, potentiation induced by aminoglycosides at NR1A/2B receptors was voltage independent. (aspetjournals.org)
  • Tolerance has been described for all available μ-opioid receptor (MOR) agonists, 1 thereby resulting in problematic long-term therapeutic use of these agents for pain control. (asahq.org)
  • Although MOR internalization has been thought to play a role in acute opioid tolerance, 3 the exposure of MORs to morphine does not cause internalization and down-regulation of these receptors, as occurs with other more potent and selective μ-opioid agonists. (asahq.org)
  • Ethanol probably acts at this receptor system. (springer.com)
  • Ethanol suppression of ventral tegmental area GABA neuron electrical transmission involves N-methyl-D-aspartate receptors. (semanticscholar.org)
  • Pepicelli O, Fedele E, Bonanno G, Raiteri M, Ajmone-Cat MA, Greco A, Levi G, Minghetti L. In vivo activation of N-methyl-D-aspartate receptors in the rat hippocampus increases prostaglandin E2 extracellular levels and triggers lipid peroxidation through cyclooxygenase-mediated mechanisms. (iss.it)
  • Furchgott RF (1972) The classification of adrenoceptors (adrenergic receptors). (springer.com)
  • Among nine genes examined, the expression of the oxytocin receptor was significantly lower in the prefrontal cortex of GluN3A KO mice than that in WT mice. (autismcandles.com)
  • To be considered pathogenic, the autoantibody should bind to an extracellular antigen (such as an ion channel or neurotransmitter receptor) and cause a functional or structural change. (nnjournal.net)
  • Neonatal receptors become restricted to perisynpatic or extrasynaptic sites, where they participate primarily in evoked currents. (pnas.org)
  • suppressed the activation of NF-B induced by HG, that was accompanied by reduced S1P2 FN and receptor expression. (paccon2016.com)
  • The role of BBR in S1P2 receptor expression regulation could associate using its inhibitory influence on NF-B activation closely. (paccon2016.com)
  • This study indicates that epigenetic DNA methylation may underlie N-methyl-D-aspartate receptor mRNA / protein expression alterations caused by isolation rearing. (bvsalud.org)