Proteins > Glutamate receptor ionotropic, NMDA 2D
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Glutamate receptor ionotropic, NMDA 2D
A glutamate receptor ionotropic, NMDA 2D that is encoded in the genome of human. [PRO:DNx, UniProtKB:O15399]
Synonyms
GluN2D;
EB11;
Glutamate [NMDA] receptor subunit epsilon-4;
N-methyl D-aspartate receptor subtype 2D;
NMDAR2D;
NR2D
Research
Bioassay Publications (27)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 7 (25.93) | 18.2507 |
| 2000's | 10 (37.04) | 29.6817 |
| 2010's | 6 (22.22) | 24.3611 |
| 2020's | 4 (14.81) | 2.80 |
Compounds (45)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| 6,7-dichloroquinoxaline-2,3-dione | Homo sapiens (human) | IC50 | 42,941.7533 | 2 | 3 |
| amantadine | Homo sapiens (human) | Ki | 10.5000 | 1 | 1 |
| arcaine | Homo sapiens (human) | IC50 | 44.5550 | 2 | 2 |
| chlorpromazine | Homo sapiens (human) | IC50 | 0.8500 | 2 | 2 |
| racemethorphan | Homo sapiens (human) | IC50 | 0.3650 | 2 | 2 |
| ifenprodil | Homo sapiens (human) | IC50 | 75.9000 | 1 | 1 |
| ketamine | Homo sapiens (human) | Ki | 0.6700 | 4 | 4 |
| kynurenic acid | Homo sapiens (human) | IC50 | 15.0000 | 1 | 1 |
| memantine | Homo sapiens (human) | Ki | 0.5400 | 2 | 2 |
| orphenadrine | Homo sapiens (human) | Ki | 6.0000 | 1 | 1 |
| procyclidine | Homo sapiens (human) | Ki | 1.7000 | 1 | 1 |
| phencyclidine | Homo sapiens (human) | Ki | 0.0324 | 3 | 3 |
| 2,3-dihydroxyquinoxaline | Homo sapiens (human) | IC50 | 51,169.4000 | 2 | 2 |
| glutamic acid | Homo sapiens (human) | IC50 | 0.0700 | 2 | 2 |
| budipine | Homo sapiens (human) | Ki | 11.7000 | 1 | 1 |
| 6,7-dichloroquinoxaline-2,3-dione | Homo sapiens (human) | IC50 | 281,171.4000 | 2 | 2 |
| pregnenolone sulfate | Homo sapiens (human) | IC50 | 118.0000 | 1 | 1 |
| ly 293558 | Homo sapiens (human) | IC50 | 12.1000 | 1 | 1 |
| besonprodil | Homo sapiens (human) | IC50 | 0.0040 | 2 | 2 |
| dizocilpine | Homo sapiens (human) | Ki | 0.0040 | 1 | 2 |
| cns 5161 | Homo sapiens (human) | Ki | 0.0019 | 1 | 1 |
| cp 101,606 | Homo sapiens (human) | IC50 | 0.0070 | 1 | 1 |
| cp 101,606 | Homo sapiens (human) | Ki | 0.0110 | 1 | 1 |
| 7-chloro-thiokynurenate | Homo sapiens (human) | IC50 | 5.0000 | 1 | 1 |
| 4-(5-(4-bromophenyl)-3-(6-methyl-2-oxo-4-phenyl-1,2-dihydroquinolin-3-yl)-4,5-dihydro-1h-pyrazol-1-yl)-4-oxobutanoic acid | Homo sapiens (human) | IC50 | 2.7000 | 2 | 2 |
| tcn 201 | Homo sapiens (human) | IC50 | 20.0000 | 2 | 2 |
| l 745870 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| levorphanol | Homo sapiens (human) | IC50 | 2.6000 | 2 | 2 |
| dextromethorphan | Homo sapiens (human) | Ki | 1.6800 | 1 | 1 |
| dextrorphan | Homo sapiens (human) | Ki | 0.2200 | 1 | 1 |
| licostinel | Homo sapiens (human) | IC50 | 2,944.2230 | 2 | 2 |
| ro 25-6981 | Homo sapiens (human) | IC50 | 0.0060 | 2 | 2 |
| ro 25-6981 | Homo sapiens (human) | Ki | 0.0058 | 2 | 2 |
| eaa-090 | Homo sapiens (human) | IC50 | 3.8150 | 2 | 2 |
| pd 174494 | Homo sapiens (human) | IC50 | 0.0040 | 1 | 1 |
| fpl 15896ar | Homo sapiens (human) | Ki | 0.5600 | 1 | 1 |
| (4-benzylpiperidin-1-yl)-(6-hydroxy-1h-indol-2-yl)methanone | Homo sapiens (human) | IC50 | 0.0120 | 1 | 1 |
| tqx 173 | Homo sapiens (human) | IC50 | 46.0000 | 1 | 1 |
| (1rs,1's)-peaqx | Homo sapiens (human) | IC50 | 0.0080 | 1 | 1 |
| nitd 609 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
Drugs with Activation Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| licostinel | Homo sapiens (human) | Kb | 0.0050 | 1 | 1 |
Repurposing of Drugs-The Ketamine Story.Journal of medicinal chemistry, , 11-25, Volume: 63, Issue:22, 2020
Ketamine esters and amides as short-acting anaesthetics: Structure-activity relationships for the side-chain.Bioorganic & medicinal chemistry, , 04-01, Volume: 27, Issue:7, 2019
Quantitative analysis of the structural requirements for blockade of the N-methyl-D-aspartate receptor at the phencyclidine binding site.Journal of medicinal chemistry, , Jan-29, Volume: 41, Issue:3, 1998
Identification of tetracyclic lactams as NMDA receptor antagonists with potential application in neurological disorders.European journal of medicinal chemistry, , May-15, Volume: 194, 2020
Methylated analogues of methyl (R)-4-(3,4-dichlorophenylacetyl)- 3-(pyrrolidin-1-ylmethyl)piperazine-1-carboxylate (GR-89,696) as highly potent kappa-receptor agonists: stereoselective synthesis, opioid-receptor affinity, receptor selectivity, and functioJournal of medicinal chemistry, , Aug-16, Volume: 44, Issue:17, 2001
Quantitative analysis of the structural requirements for blockade of the N-methyl-D-aspartate receptor at the phencyclidine binding site.Journal of medicinal chemistry, , Jan-29, Volume: 41, Issue:3, 1998
(3SR,4aRS,6RS,8aRS)-6-[2-(1H-tetrazol-5-yl)ethyl]decahydroisoquinoline-3 - carboxylic acid: a structurally novel, systemically active, competitive AMPA receptor antagonist.Journal of medicinal chemistry, , Jul-09, Volume: 36, Issue:14, 1993
Oxamides as novel NR2B selective NMDA receptor antagonists.Bioorganic & medicinal chemistry letters, , Aug-02, Volume: 14, Issue:15, 2004
Indole-2-carboxamides as novel NR2B selective NMDA receptor antagonists.Bioorganic & medicinal chemistry letters, , Nov-03, Volume: 13, Issue:21, 2003
Oxamides as novel NR2B selective NMDA receptor antagonists.Bioorganic & medicinal chemistry letters, , Aug-02, Volume: 14, Issue:15, 2004
2-(3,4-Dihydro-1H-isoquinolin-2yl)-pyridines as a novel class of NR1/2B subtype selective NMDA receptor antagonists.Bioorganic & medicinal chemistry letters, , Mar-10, Volume: 13, Issue:5, 2003
Positive and Negative Allosteric Modulators of N-Methyl-d-aspartate (NMDA) Receptors: Structure-Activity Relationships and Mechanisms of Action.Journal of medicinal chemistry, , 01-10, Volume: 62, Issue:1, 2019
Structure-activity relationships and pharmacophore model of a noncompetitive pyrazoline containing class of GluN2C/GluN2D selective antagonists.Journal of medicinal chemistry, , Aug-22, Volume: 56, Issue:16, 2013
CoMFA and homology-based models of the glycine binding site of N-methyl-d-aspartate receptor.Journal of medicinal chemistry, , Apr-24, Volume: 46, Issue:9, 2003
The glycine site on the NMDA receptor: structure-activity relationships and therapeutic potential.Journal of medicinal chemistry, , Nov-25, Volume: 37, Issue:24, 1994
Oxamides as novel NR2B selective NMDA receptor antagonists.Bioorganic & medicinal chemistry letters, , Aug-02, Volume: 14, Issue:15, 2004
2-(3,4-Dihydro-1H-isoquinolin-2yl)-pyridines as a novel class of NR1/2B subtype selective NMDA receptor antagonists.Bioorganic & medicinal chemistry letters, , Mar-10, Volume: 13, Issue:5, 2003
Indole-2-carboxamides as novel NR2B selective NMDA receptor antagonists.Bioorganic & medicinal chemistry letters, , Nov-03, Volume: 13, Issue:21, 2003
Discovery of (R)-1-[2-hydroxy-3-(4-hydroxy-phenyl)-propyl]-4-(4-methyl-benzyl)-piperidin-4-ol: a novel NR1/2B subtype selective NMDA receptor antagonist.Bioorganic & medicinal chemistry letters, , Aug-20, Volume: 11, Issue:16, 2001
Enables
This protein enables 8 target(s):
| Target | Category | Definition |
|---|
| glutamate-gated receptor activity | molecular function | Catalysis of the transmembrane transfer of an ion by a channel that opens when glutamate has been bound by the channel complex or one of its constituent parts. [ISBN:0198506732] |
| NMDA glutamate receptor activity | molecular function | An cation channel that opens in response to binding by extracellular glutmate, but only if glycine is also bound and the membrane is depolarized. Voltage gating is indirect, due to ejection of bound magnesium from the pore at permissive voltages. [GOC:mah, PMID:10049997] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| glutamate binding | molecular function | Binding to glutamate, the anion of 2-aminopentanedioic acid. [GOC:ai] |
| voltage-gated monoatomic cation channel activity | molecular function | Enables the transmembrane transfer of a cation by a voltage-gated channel. A cation is a positively charged ion. A voltage-gated channel is a channel whose open state is dependent on the voltage across the membrane in which it is embedded. [GOC:mtg_transport, ISBN:0815340729] |
| glutamate-gated calcium ion channel activity | molecular function | Enables the transmembrane transfer of a calcium ion by a channel that opens when glutamate has been bound by the channel complex or one of its constituent parts. [GOC:mtg_transport, ISBN:0815340729] |
| ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potential | molecular function | Any ligand-gated ion channel activity, occurring in the presynaptic membrane, that is involved in regulation of presynaptic membrane potential. [GOC:dos, PMID:15145529, PMID:19558451] |
| transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential | molecular function | Any transmitter-gated ion channel activity that is involved in regulation of postsynaptic membrane potential. [GO_REF:0000061, GOC:TermGenie, PMID:20200227] |
Located In
This protein is located in 6 target(s):
| Target | Category | Definition |
|---|
| endoplasmic reticulum membrane | cellular component | The lipid bilayer surrounding the endoplasmic reticulum. [GOC:mah] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| postsynaptic membrane | cellular component | A specialized area of membrane facing the presynaptic membrane on the tip of the nerve ending and separated from it by a minute cleft (the synaptic cleft). Neurotransmitters cross the synaptic cleft and transmit the signal to the postsynaptic membrane. [ISBN:0198506732] |
| presynaptic active zone membrane | cellular component | The membrane portion of the presynaptic active zone; it is the site where docking and fusion of synaptic vesicles occurs for the release of neurotransmitters. [PMID:12812759, PMID:12923177, PMID:3152289] |
| hippocampal mossy fiber to CA3 synapse | cellular component | One of the giant synapses that form between the mossy fiber axons of dentate gyrus granule cells and the large complex spines of CA3 pyramidal cells. It consists of a giant bouton known as the mossy fiber expansion, synapsed to the complex, multiheaded spine (thorny excresence) of a CA3 pyramidal cell. [DOI:10.1002/1096-9861, PMID:13869693, PMID:23264762] |
| glutamatergic synapse | cellular component | A synapse that uses glutamate as a neurotransmitter. [GOC:dos] |
Active In
This protein is active in 2 target(s):
| Target | Category | Definition |
|---|
| postsynaptic density membrane | cellular component | The membrane component of the postsynaptic density. This is the region of the postsynaptic membrane in which the population of neurotransmitter receptors involved in synaptic transmission are concentrated. [GOC:dos] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
Part Of
This protein is part of 1 target(s):
| Target | Category | Definition |
|---|
| NMDA selective glutamate receptor complex | cellular component | An assembly of four or five subunits which form a structure with an extracellular N-terminus and a large loop that together form the ligand binding domain. The C-terminus is intracellular. The ionotropic glutamate receptor complex itself acts as a ligand gated ion channel; on binding glutamate, charged ions pass through a channel in the center of the receptor complex. NMDA receptors are composed of assemblies of NR1 subunits (Figure 3) and NR2 subunits, which can be one of four separate gene products (NR2A-D). Expression of both subunits are required to form functional channels. The glutamate binding domain is formed at the junction of NR1 and NR2 subunits. NMDA receptors are permeable to calcium ions as well as being permeable to other ions. Thus NMDA receptor activation leads to a calcium influx into the post-synaptic cells, a signal thought to be crucial for the induction of NMDA-receptor dependent LTP and LTD. [http://www.bris.ac.uk/Depts/Synaptic/info/glutamate.html] |
Involved In
This protein is involved in 19 target(s):
| Target | Category | Definition |
|---|
| startle response | biological process | An action or movement due to the application of a sudden unexpected stimulus. [GOC:dph] |
| brain development | biological process | The process whose specific outcome is the progression of the brain over time, from its formation to the mature structure. Brain development begins with patterning events in the neural tube and ends with the mature structure that is the center of thought and emotion. The brain is responsible for the coordination and control of bodily activities and the interpretation of information from the senses (sight, hearing, smell, etc.). [GOC:dph, GOC:jid, GOC:tb, UBERON:0000955] |
| adult locomotory behavior | biological process | Locomotory behavior in a fully developed and mature organism. [GOC:ai] |
| calcium-mediated signaling | biological process | Any intracellular signal transduction in which the signal is passed on within the cell via calcium ions. [GOC:signaling] |
| ionotropic glutamate receptor signaling pathway | biological process | The series of molecular signals initiated by glutamate binding to a glutamate receptor on the surface of the target cell, followed by the movement of ions through a channel in the receptor complex, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:signaling, ISBN:0198506732] |
| regulation of synaptic plasticity | biological process | A process that modulates synaptic plasticity, the ability of synapses to change as circumstances require. They may alter function, such as increasing or decreasing their sensitivity, or they may increase or decrease in actual numbers. [GOC:dph, GOC:jid, GOC:tb, PMID:11891290] |
| regulation of neuronal synaptic plasticity | biological process | A process that modulates neuronal synaptic plasticity, the ability of neuronal synapses to change as circumstances require. They may alter function, such as increasing or decreasing their sensitivity, or they may increase or decrease in actual numbers. [GOC:jid, PMID:11891290] |
| regulation of sensory perception of pain | biological process | Any process that modulates the frequency, rate or extent of the sensory perception of pain, the series of events required for an organism to receive a painful stimulus, convert it to a molecular signal, and recognize and characterize the signal. [GOC:ai] |
| positive regulation of synaptic transmission, glutamatergic | biological process | Any process that activates, maintains or increases the frequency, rate or extent of glutamatergic synaptic transmission, the process of communication from a neuron to another neuron across a synapse using the neurotransmitter glutamate. [GOC:ai] |
| calcium ion transmembrane import into cytosol | biological process | A process in which a calcium ion is transported from one side of a membrane to the other into the cytosol by means of some agent such as a transporter or pore. [GOC:vw] |
| monoatomic cation transmembrane transport | biological process | The process in which a monoatomic cation is transported across a membrane. Monatomic cations (also called simple cations) are positively charged ions consisting of exactly one atom. [GOC:dos, GOC:vw] |
| excitatory chemical synaptic transmission | biological process | Synaptic transmission that results in an excitatory postsynaptic potential. [GOC:dos] |
| regulation of presynaptic membrane potential | biological process | Any process that modulates the potential difference across a presynaptic membrane. [GOC:dph, GOC:ef] |
| regulation of monoatomic cation transmembrane transport | biological process | Any process that modulates the frequency, rate or extent of cation transmembrane transport. [GO_REF:0000058, GOC:TermGenie, PMID:15304482] |
| cellular response to L-glutamate | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a L-glutamate(1-) stimulus. [GO_REF:0000071, GOC:TermGenie, PMID:25962137] |
| positive regulation of excitatory postsynaptic potential | biological process | Any process that enhances the establishment or increases the extent of the excitatory postsynaptic potential (EPSP) which is a temporary increase in postsynaptic potential due to the flow of positively charged ions into the postsynaptic cell. The flow of ions that causes an EPSP is an excitatory postsynaptic current (EPSC) and makes it easier for the neuron to fire an action potential. [GOC:bf, GOC:BHF] |
| synaptic transmission, glutamatergic | biological process | The vesicular release of glutamate from a presynapse, across a chemical synapse, the subsequent activation of glutamate receptors at the postsynapse of a target cell (neuron, muscle, or secretory cell) and the effects of this activation on the postsynaptic membrane potential and ionic composition of the postsynaptic cytosol. This process encompasses both spontaneous and evoked release of neurotransmitter and all parts of synaptic vesicle exocytosis. Evoked transmission starts with the arrival of an action potential at the presynapse. [GOC:dos] |
| excitatory postsynaptic potential | biological process | A process that leads to a temporary increase in postsynaptic potential due to the flow of positively charged ions into the postsynaptic cell. The flow of ions that causes an EPSP is an excitatory postsynaptic current (EPSC) and makes it easier for the neuron to fire an action potential. [GOC:dph, GOC:ef] |
| long-term synaptic potentiation | biological process | A process that modulates synaptic plasticity such that synapses are changed resulting in the increase in the rate, or frequency of synaptic transmission at the synapse. [GOC:dgh, GOC:dph] |