Distinct functional and pharmacological properties of Triheteromeric GluN1/GluN2A/GluN2B NMDA receptors.

No abstract is available for this paper.

• Publication year

  2014

• Venue

  Neuron

• Publication date

  2014-03-05

• Fields of study

  Biology, Medicine

• Identifiers
  DOI 10.1016/j.neuron.2014.01.035PMID 24607230PMCID PMC3957490
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Diversity in NMDA Receptor Composition

  2013cited by this paper
• Structural Determinants of Agonist Efficacy at the Glutamate Binding Site of N-Methyl-d-Aspartate Receptors

  2013influential reference
• NMDA receptor subunit diversity: impact on receptor properties, synaptic plasticity and disease

  2013influential reference
• Effect of Ifenprodil on GluN1/GluN2B N-Methyl-D-aspartate Receptor Gating

  2013cited by this paper
• Triheteromeric NMDA Receptors at Hippocampal Synapses

  2013influential reference
• Influence of the intracellular GluN2 C-terminal domain on NMDA receptor function.

  2012cited by this paper
• Amino-Terminal Ligands Prolong NMDA Receptor-Mediated EPSCs

  2012cited by this paper
• C-terminal Domains of N-Methyl-d-aspartic Acid Receptor Modulate Unitary Channel Conductance and Gating*

  2012cited by this paper
• Mapping the Binding of GluN2B-Selective N-Methyl-d-aspartate Receptor Negative Allosteric Modulators

  2012influential reference
• Subunit-Selective Allosteric Inhibition of Glycine Binding to NMDA Receptors

  2012cited by this paper
• The Neurophysiology and Pathology of Brain Zinc

  2011influential reference
• Distinct modes of AMPA receptor suppression at developing synapses by GluN2A and GluN2B: single-cell NMDA receptor subunit deletion in vivo.

  2011influential reference
• Zinc alleviates pain through high-affinity binding to the NMDA receptor NR2A subunit

  2011cited by this paper
• Subunit Arrangement and Phenylethanolamine Binding in GluN1/GluN2B NMDA Receptors

  2011influential reference
• Glutamate receptor dynamics and protein interaction: lessons from the NMDA receptor.

  2011cited by this paper
• Glutamate Receptor Ion Channels: Structure, Regulation, and Function

  2010influential reference
• Identification and Characterization of Novel NMDA Receptor Antagonists Selective for NR2A- over NR2B-Containing Receptors

  2010cited by this paper
• Triheteromeric NR1/NR2A/NR2B Receptors Constitute the Major N-Methyl-d-aspartate Receptor Population in Adult Hippocampal Synapses

  2010cited by this paper
• Novel Approach to Probe Subunit-specific Contributions to N-Methyl-d-aspartate (NMDA) Receptor Trafficking Reveals a Dominant Role for NR2B in Receptor Recycling*

  2010cited by this paper
• Structure of the zinc‐bound amino‐terminal domain of the NMDA receptor NR2B subunit

  2009influential reference
• Zinc inhibition of rat NR1/NR2A N‐methyl‐d‐aspartate receptors

  2008cited by this paper
• An Innovative Design to Establish Proof of Concept of the Antidepressant Effects of the NR2B Subunit Selective N-Methyl-D-Aspartate Antagonist, CP-101,606, in Patients With Treatment-Refractory Major Depressive Disorder

  2008cited by this paper
• NMDA Di-Heteromeric Receptor Populations and Associated Proteins in Rat Hippocampus

  2007cited by this paper
• Subunit-Specific Agonist Activity at NR2A-, NR2B-, NR2C-, and NR2D-Containing N-Methyl-d-aspartate Glutamate Receptors

  2007cited by this paper
• Tweaking Agonist Efficacy at N-Methyl-d-aspartate Receptors by Site-Directed Mutagenesis

  2005cited by this paper
• Functional NR2B‐ and NR2D‐containing NMDA receptor channels in rat substantia nigra dopaminergic neurones

  2005cited by this paper
• Modulation of triheteromeric NMDA receptors by N-terminal domain ligands.

  2005influential reference
• Allosteric interaction between zinc and glutamate binding domains on NR2A causes desensitization of NMDA receptors

  2005cited by this paper
• Assembly-dependent surface targeting of the heterodimeric GABAB Receptor is controlled by COPI but not 14-3-3.

  2005influential reference
• The Micromolar Zinc-Binding Domain on the NMDA Receptor Subunit NR2B

  2005influential reference
• Molecular Structure and Physiological Functions of GABAB Receptors

  2004cited by this paper
• Molecular structure and physiological functions of GABA(B) receptors.

  2004cited by this paper
• Conformations of variably linked chimeric proteins evaluated by synchrotron X‐ray small‐angle scattering

  2004cited by this paper
• Closed state of both binding domains of homodimeric mGlu receptors is required for full activity

  2004influential reference
• NR2B and NR2D Subunits Coassemble in Cerebellar Golgi Cells to Form a Distinct NMDA Receptor Subtype Restricted to Extrasynaptic Sites

  2003cited by this paper
• Subtypes of NMDA receptors in new‐born rat hippocampal granule cells

  2002cited by this paper
• Analysis of endoplasmic reticulum trafficking signals by combinatorial screening in mammalian cells.

  2001cited by this paper
• Molecular organization of a zinc binding n-terminal modulatory domain in a NMDA receptor subunit.

  2000cited by this paper
• A trafficking checkpoint controls GABA(B) receptor heterodimerization.

  2000cited by this paper
• Molecular determinants of coordinated proton and zinc inhibition of N-methyl-D-aspartate NR1/NR2A receptors.

  2000influential reference
• Developmental Profile of the Changing Properties of NMDA Receptors at Cerebellar Mossy Fiber–Granule Cell Synapses

  2000cited by this paper
• The Incorporation of NMDA Receptors with a Distinct Subunit Composition at Nascent Hippocampal Synapses In Vitro

  1999cited by this paper
• Heterodimerization of a functional GABAB receptor is mediated by parallel coiled-coil alpha-helices.

  1999cited by this paper
• Identification and mechanism of action of two histidine residues underlying high-affinity Zn2+ inhibition of the NMDA receptor.

  1999cited by this paper
• Control of Voltage-Independent Zinc Inhibition of NMDA Receptors by the NR1 Subunit

  1998influential reference
• Increased contribution of NR2A subunit to synaptic NMDA receptors in developing rat cortical neurons

  1998cited by this paper
• Functional and pharmacological differences between recombinant N-methyl-D-aspartate receptors.

  1998influential reference
• Identification of Amino Acid Residues of the NR2A Subunit That Control Glutamate Potency in Recombinant NR1/NR2A NMDA Receptors

  1998cited by this paper
• Developmental Changes in NMDA Receptor Glycine Affinity and Ifenprodil Sensitivity Reveal Three Distinct Populations of NMDA Receptors in Individual Rat Cortical Neurons

  1998cited by this paper
• Molecular Dissection of Native Mammalian Forebrain NMDA Receptors Containing the NR1 C2 Exon: Direct Demonstration of NMDA Receptors Comprising NR1, NR2A, and NR2B Subunits Within the Same Complex

  1997cited by this paper
• High-Affinity Zinc Inhibition of NMDA NR1–NR2A Receptors

  1997influential reference
• Molecular determinants of agonist discrimination by NMDA receptor subunits: analysis of the glutamate binding site on the NR2B subunit.

  1997cited by this paper
• The majority of N-methyl-D-aspartate receptor complexes in adult rat cerebral cortex contain at least three different subunits (NR1/NR2A/NR2B).

  1997influential reference
• NR2A Subunit Expression Shortens NMDA Receptor Synaptic Currents in Developing Neocortex

  1997cited by this paper
• Separating dual effects of zinc at recombinant N-methyl-D-aspartate receptors.

  1996influential reference
• A novel mechanism of activity‐dependent NMDA receptor antagonism describes the effect of ifenprodil in rat cultured cortical neurones.

  1996cited by this paper
• Synaptic NMDA receptors in developing mouse hippocampal neurones: functional properties and sensitivity to ifenprodil.

  1996cited by this paper
• Changing subunit composition of heteromeric NMDA receptors during development of rat cortex

  1994cited by this paper
• Molecular characterization of N-methyl-D-aspartate receptors expressed in mammalian cells yields evidence for the coexistence of three subunit types within a discrete receptor molecule.

  1994influential reference
• Kinetic analysis of antagonist action at N-methyl-D-aspartic acid receptors. Two binding sites each for glutamate and glycine.

  1991cited by this paper
• Activation kinetics reveal the number of glutamate and glycine binding sites on the N-methyl-D-aspartate receptor.

  1991cited by this paper
• Channel kinetics determine the time course of NMDA receptor-mediated synaptic currents

  1990cited by this paper

• Mice carrying a GluN2B protein-truncating variant have altered NMDA receptor subunit composition and their behavior recapitulates patient phenotypes

  2026influential citation
• A GluN2B disease-associated variant promotes the degradation of NMDA receptors via autophagy

  2026cites this paper
• GluN2D NMDARs: Bridging Physiology and Pathology.

  2026cites this paper
• Novel binding mode for negative allosteric NMDA receptor modulators.

  2026cites this paper
• Conformational diversity and fully opening mechanism of native NMDA receptor.

  2026cites this paper
• UCM-A86 is a selective positive allosteric modulator of GluN1/GluN3 NMDA receptors.

  2026cites this paper
• Design of (R)-3-(5-Thienyl)carboxamido-2-aminopropanoic Acid Derivatives as Novel NMDA Receptor Glycine Site Agonists: Variation in Molecular Geometry to Improve Potency and Augment GluN2 Subunit-Specific Activity

  2025cites this paper
• CaMKII monomers are sufficient for GluN2B binding, co-condensation, and synaptic potentiation

  2025cites this paper
• Optochemical profiling of NMDAR molecular diversity at synaptic and extrasynaptic sites

  2025influential citation
• Inhibition of GluN2B-containing N-methyl-d-aspartate receptors by radiprodil.

  2025cites this paper
• Emerging Roles of GluN3B NMDA Receptor Subunit in the Central Nervous System

  2025cites this paper
• GluN2A-NMDA receptor inhibition disinhibits the prefrontal cortex, reduces forced swim immobility, and impairs sensorimotor gating

  2025cites this paper
• Imaging and Quantifying the Diversity of Native NMDA Receptors

  2025cites this paper
• UCM-A86 is a selective positive allosteric modulator of GluN1/GluN3 NMDA receptors

  2025cites this paper
• Selective enhancement of the interneuron network and gamma‐band power via GluN2C/GluN2D NMDA receptor potentiation

  2025influential citation
• Assembly and architecture of endogenous NMDA receptors in adult cerebral cortex and hippocampus.

  2025cites this paper
• A genetically encoded secreted toxin potentiates synaptic NMDA receptors in hippocampal neurons and confers neuroprotection

  2025cites this paper
• Pharmacological characterisation of JNJ‐78911118, a novel, centrally‐penetrant, selective GluN2A antagonist

  2025cites this paper
• Enhancement of hippocampal interneuron excitability by NMDA receptor positive allosteric modulation

  2025cites this paper
• Future Perspectives of NMDAR in CNS Disorders

  2025cites this paper
• Inhibition of NMDA receptors and other ion channel types by membrane-associated drugs

  2025cites this paper
• New advances in small molecule drugs targeting NMDA receptors

  2025influential citation
• Trans-synaptic molecular context of NMDA receptor nanodomains

  2025cites this paper
• The Astrocytic Zinc Transporter ZIP12 Is a Synaptic Protein That Contributes to Synaptic Zinc Levels in the Mouse Auditory Cortex

  2025cites this paper
• Discovery of Brain-Penetrative Negative Allosteric Modulators of NMDA Receptors Using FEP-Guided Structure Optimization and Membrane Permeability Prediction

  2025cites this paper
• The effect of caffeine in a model of schizophrenia-like behavior induced by MK-801 in mice.

  2025cites this paper
• Disruption of grin2A, an Epilepsy-Associated Gene, Produces Altered Spontaneous Swim Behavior in Zebrafish

  2025cites this paper
• Structural Basis of Inhibition and Desensitization in Heteromeric Kainate Receptors

  2025cites this paper
• Damage to N-methyl D-aspartate receptors following perinatal hypoxia-ischemia and its relation to schizophrenia

  2025cites this paper
• EAR-20 peptide, a novel NMDA receptor positive allosteric modulator

  2025cites this paper
• Structural prediction of GluN3 NMDA receptors

  2024cites this paper
• Zelquistinel acts at an extracellular binding domain to modulate intracellular calcium inactivation of N-methyl-D-aspartate receptors.

  2024cites this paper
• Characterization of Mice Carrying a Neurodevelopmental Disease-Associated GluN2B(L825V) Variant

  2024cites this paper
• Reversible Control of Native GluN2B-Containing NMDA Receptors with Visible Light

  2024cites this paper
• D-Amino acids from foods and gut microbiota and their effects in health and disease

  2024cites this paper
• Early Expression of GluN2A-Containing NMDA Receptors in A Model of Fragile X Syndrome.

  2024cites this paper
• Characterizing Functional Contributions of Specific GluN2 Subunits to Individual Postsynaptic NMDAR Responses Using Biophysical Parameters.

  2024cites this paper
• Incremental induction of NMDAR-STP and NMDAR-LTP in the CA1 area of ventral hippocampal slices relies on graded activation of discrete NMDA receptors

  2024cites this paper
• Disease-Associated Variants in GRIN1, GRIN2A and GRIN2B genes: Insights into NMDA Receptor Structure, Function, and Pathophysiology.

  2024cites this paper
• Regulation of NMDAR activation efficiency by environmental factors and subunit composition

  2024influential citation
• Rescuing tri-heteromeric NMDA receptor function: the potential of pregnenolone-sulfate in loss-of-function GRIN2B variants

  2024cites this paper
• Selective Cell-Surface Expression of Triheteromeric NMDA Receptors.

  2024influential citation
• GluN2A: A Promising Target for Developing Novel Antidepressants

  2024influential citation
• Comprehensive investigation of multiple targets in the development of newer drugs for the Alzheimer's disease

  2024cites this paper
• Evaluation of allosteric NMDA receptor modulation by GluN2A-selective antagonists using pharmacological equilibrium modeling.

  2024cites this paper
• GlyT1 inhibition promotes neuroprotection in the middle cerebral artery occlusion model through the activation of GluN2A-containing NMDAR.

  2024cites this paper
• Selective Enhancement of the Interneuron Network and Gamma-Band Power via GluN2C/GluN2D NMDA Receptor Potentiation

  2024cites this paper
• The NMDA receptor antagonists memantine and ketamine as anti-migraine agents

  2023cites this paper
• Rescue of synaptic and cognitive functions in polysialic acid-deficient mice and dementia models by short polysialic acid fragments.

  2023cites this paper
• Targeting NMDA receptor signaling for therapeutic intervention in brain disorders

  2023cites this paper
• In the fast lane: Receptor trafficking during status epilepticus

  2023cites this paper
• Reduced expression of GluN2A induces a delay in neuron maturation

  2023cites this paper
• Attenuation of Vanadium-Induced Neurotoxicity in Rat Hippocampal Slices (In Vitro) and Mice (In Vivo) by ZA-II-05, a Novel NMDA-Receptor Antagonist

  2023cites this paper
• Novel GluN2B-Selective NMDA Receptor Negative Allosteric Modulator Possesses Intrinsic Analgesic Properties and Enhances Analgesia of Morphine in a Rodent Tail Flick Pain Model

  2023cites this paper
• Calcium and Calmodulin-dependent Inhibition of NMDA Receptor Currents.

  2023cites this paper
• Trans-synaptic molecular context of NMDA receptor nanodomains

  2023cites this paper
• The Role of NMDA Receptor Subunits in the Effect of Memantine on the Brain of Healthy Animals

  2023cites this paper
• Therapeutic potential of N-methyl-D-aspartate receptor modulators in psychiatry

  2023cites this paper
• Early life stress lastingly alters the function and AMPA‐receptor composition of glutamatergic synapses in the hippocampus of male mice

  2023cites this paper
• The role of N-methyl-D-aspartate glutamate receptors in Alzheimer's disease: from pathophysiology to therapeutic approaches.

  2023cites this paper
• Reversible inhibition of GluN2B-containing NMDA receptors with an in situ red-shifted, photoswitchable antagonist

  2023cites this paper
• β2-microglobulin functions as an endogenous NMDAR antagonist to impair synaptic function.

  2023cites this paper
• Structural insights into NMDA receptor pharmacology

  2023cites this paper
• Heterogeneity of synaptic NMDA receptor responses within individual lamina I pain processing neurons across sex in rats and humans

  2023influential citation
• Extrasynaptic NMDA receptors in acute and chronic excitotoxicity: implications for preventive treatments of ischemic stroke and late-onset Alzheimer’s disease

  2023cites this paper
• The t-N-methyl-d-aspartate receptor: Making the case for d-Serine to be considered its inverse co-agonist.

  2023cites this paper
• Synaptic zinc potentiates AMPA receptor function in mouse auditory cortex

  2023cites this paper
• GluN2B-containing NMDARs in the mammalian brain: pharmacology, physiology, and pathology

  2023influential citation
• Medial septum glutamatergic neurons modulate nociception in chronic neuropathic pain via projections to lateral hypothalamus

  2023cites this paper
• Pharmacological Potential of 3-Benzazepines in NMDAR-Linked Pathophysiological Processes

  2023cites this paper
• CNS4 causes subtype‐specific changes in agonist efficacy and reversal potential of permeant cations in NMDA receptors

  2023cites this paper
• Differential regulation of tetramerization of the AMPA receptor glutamate–gated ion channel by auxiliary subunits

  2023cites this paper
• GluN2A and GluN2B N-Methyl-D-Aspartate Receptor (NMDARs) Subunits: Their Roles and Therapeutic Antagonists in Neurological Diseases

  2023cites this paper
• Disturbance of glutamate metabolism and inhibition of CaM-CaMKII-CREB signaling pathway in the hippocampus of mice induced by 1,2-dichloroethane exposure.

  2022cites this paper
• Discovery of (R)-2-amino-3-triazolpropanoic acid derivatives as NMDA receptor glycine site agonists with GluN2 subunit-specific activity

  2022cites this paper
• In vitro ADME characterization of a very potent 3-acylamino-2-aminopropionic acid-derived GluN2C-NMDA receptor agonist and its ester prodrugs

  2022cites this paper
• Two extreme Loss-of-Function GRIN2B-mutations are detrimental to tri-heteromeric NMDAR-function, but rescued by pregnanolone-sulfate

  2022cites this paper
• Synaptic NMDA receptor activity at resting membrane potentials

  2022cites this paper
• Protein quality control of N-methyl-D-aspartate receptors

  2022cites this paper
• Activation of non-classical NMDA receptors by glycine impairs barrier function of brain endothelial cells

  2022cites this paper
• Therapeutic Potential of Quercetin and its Derivatives in Epilepsy: Evidence from Preclinical Studies

  2022cites this paper
• Biphenyl scaffold for the design of NMDA-receptor negative modulators: molecular modeling, synthesis, and biological activity.

  2022cites this paper
• miR-146a and miR-200b alter cognition by targeting NMDA receptor subunits

  2022cites this paper
• Ghrelin-O-acyltransferase (GOAT) acylates ghrelin in the hippocampus.

  2022cites this paper
• Progresses in GluN2A-containing NMDA Receptors and their Selective Regulators

  2022cites this paper
• Opportunities for Precision Treatment of GRIN2A and GRIN2B Gain-of-Function Variants in Triheteromeric N-Methyl-D-Aspartate Receptors

  2022influential citation
• Development and characterization of functional antibodies targeting NMDA receptors

  2022cites this paper
• Changes in NMDA Receptor Function in Rapid Ischemic Tolerance: A Potential Role for Tri-Heteromeric NMDA Receptors

  2022cites this paper
• Synaptic Dysfunction by Mutations in GRIN2B: Influence of Triheteromeric NMDA Receptors on Gain-of-Function and Loss-of-Function Mutant Classification

  2022influential citation
• Dose-dependent suppression of hippocampal contextual memory formation, place cells, and spatial engrams by the NMDAR antagonist (R)-CPP

  2022cites this paper
• Atypical NMDA Receptors Limit Synaptic Plasticity in the Adult Ventral Hippocampus

  2022cites this paper
• A Mechanistic Model of NMDA and AMPA Receptor-Mediated Synaptic Transmission in Individual Hippocampal CA3-CA1 Synapses: A Computational Multiscale Approach

  2021cites this paper
• Rapid effects of neurosteroids on neuronal plasticity and their physiological and pathological implications.

  2021cites this paper
• Specific pathogenic mutations in the M3 domain of the GluN1 subunit regulate the surface delivery and pharmacological sensitivity of NMDA receptors.

  2021cites this paper
• Behind the scenes: Are latent memories supported by calcium independent plasticity?

  2021cites this paper
• Structure, Function, and Pharmacology of Glutamate Receptor Ion Channels

  2021cites this paper
• Derivatives of (R)-3-(5-Furanyl)carboxamido-2-aminopropanoic Acid as Potent NMDA Receptor Glycine Site Agonists with GluN2 Subunit-Specific Activity.

  2021cites this paper
• Allosteric antagonist action at triheteromeric NMDA receptors

  2021cites this paper
• Positive allosteric modulation of NMDA receptors: mechanisms, physiological impact and therapeutic potential

  2021cites this paper
• 21st Century Excitatory Amino Acid Research: a Q &A with Jeff Watkins and Dick Evans.

  2021cites this paper