Glutamate receptor ionotropic, NMDA 2A

A glutamate receptor ionotropic, NMDA 2A that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q12879]

Synonyms

GluN2A;
Glutamate [NMDA] receptor subunit epsilon-1;
N-methyl D-aspartate receptor subtype 2A;
NMDAR2A;
NR2A;
hNR2A

Research

Bioassay Publications (41)

Timeframe	Studies on this Protein(%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	7 (17.07)	18.2507
2000's	11 (26.83)	29.6817
2010's	16 (39.02)	24.3611
2020's	7 (17.07)	2.80

Compounds (55)

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
tacrine	Homo sapiens (human)	IC50	25.8750	4	4
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	39.5000	1	1
ketamine	Homo sapiens (human)	IC50	3.5563	3	3
ketamine	Homo sapiens (human)	Ki	0.5720	5	5
kynurenic acid	Homo sapiens (human)	IC50	15.0000	1	1
memantine	Homo sapiens (human)	IC50	3.6620	6	6
memantine	Homo sapiens (human)	Ki	0.5400	2	2
methoctramine	Homo sapiens (human)	IC50	0.1380	1	1
orphenadrine	Homo sapiens (human)	Ki	6.0000	1	1
pentamidine	Homo sapiens (human)	IC50	0.7200	1	1
procyclidine	Homo sapiens (human)	Ki	1.7000	1	1
phencyclidine	Homo sapiens (human)	IC50	0.2050	2	2
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
ly 293558	Homo sapiens (human)	IC50	12.1000	1	1
besonprodil	Homo sapiens (human)	IC50	0.0040	2	2
philanthotoxin 343	Homo sapiens (human)	IC50	2.7390	1	1
dizocilpine	Homo sapiens (human)	IC50	0.0290	1	1
dizocilpine	Homo sapiens (human)	Ki	0.0040	1	2
memantine hydrochloride	Homo sapiens (human)	IC50	2.3000	1	1
esketamine	Homo sapiens (human)	IC50	0.0114	1	1
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
dexoxadrol	Homo sapiens (human)	IC50	0.0097	1	1
dexoxadrol	Homo sapiens (human)	Ki	0.0190	1	1
7-chloro-thiokynurenate	Homo sapiens (human)	IC50	5.0000	1	1
tcn 201	Homo sapiens (human)	IC50	0.2198	4	4
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)	IC50	1.3000	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	17.3373	3	3
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	0.1390	2	2
etoxadrol	Homo sapiens (human)	Ki	0.0220	1	1
methoxydine	Homo sapiens (human)	IC50	3.9811	1	1
nitd 609	Homo sapiens (human)	IC50	10.0000	1	1

Drugs with Activation Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
clofibric acid	Homo sapiens (human)	EC50	300.0000	1	1
bezafibrate	Homo sapiens (human)	EC50	60.0000	1	1
fenofibric acid	Homo sapiens (human)	EC50	300.0000	1	1
25-hydroxycholesterol	Homo sapiens (human)	EC50	10.0000	1	1
rosiglitazone	Homo sapiens (human)	EC50	0.0210	1	1
pregnenolone sulfate	Homo sapiens (human)	EC50	27.5000	2	2
24-hydroxycholesterol	Homo sapiens (human)	EC50	0.2000	3	3
(3-chlorophenyl)(6,7-dimethoxy-1-((4-methoxyphenoxy)methyl)-3,4-dihydroisoquinolin-2(1h)-yl)methanone	Homo sapiens (human)	EC50	10.0000	1	1
gw 9578	Homo sapiens (human)	EC50	1.0000	1	1

Drugs with Other Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
licostinel	Homo sapiens (human)	Kb	0.0050	1	1

Enables

This protein enables 6 target(s):

Target	Category	Definition
amyloid-beta binding	molecular function	Binding to an amyloid-beta peptide/protein. [GOC:hjd]
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]
zinc ion binding	molecular function	Binding to a zinc ion (Zn). [GOC:ai]
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]
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 11 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]
synaptic vesicle	cellular component	A secretory organelle, typically 50 nm in diameter, of presynaptic nerve terminals; accumulates in high concentrations of neurotransmitters and secretes these into the synaptic cleft by fusion with the 'active zone' of the presynaptic plasma membrane. [PMID:10099709, PMID:12563290]
cell surface	cellular component	The external part of the cell wall and/or plasma membrane. [GOC:jl, GOC:mtg_sensu, GOC:sm]
postsynaptic density	cellular component	An electron dense network of proteins within and adjacent to the postsynaptic membrane of an asymmetric, neuron-neuron synapse. Its major components include neurotransmitter receptors and the proteins that spatially and functionally organize them such as anchoring and scaffolding molecules, signaling enzymes and cytoskeletal components. [GOC:BHF, GOC:dos, GOC:ef, GOC:jid, GOC:pr, GOC:sjp, http://molneuro.kaist.ac.kr/psd, PMID:14532281, Wikipedia:Postsynaptic_density]
cytoplasmic vesicle membrane	cellular component	The lipid bilayer surrounding a cytoplasmic vesicle. [GOC:mah]
presynaptic membrane	cellular component	A specialized area of membrane of the axon terminal that faces the plasma membrane of the neuron or muscle fiber with which the axon terminal establishes a synaptic junction; many synaptic junctions exhibit structural presynaptic characteristics, such as conical, electron-dense internal protrusions, that distinguish it from the remainder of the axon plasma membrane. [GOC:jl, ISBN:0815316194]
dendritic spine	cellular component	A small, membranous protrusion from a dendrite that forms a postsynaptic compartment, typically receiving input from a single presynapse. They function as partially isolated biochemical and an electrical compartments. Spine morphology is variable:they can be thin, stubby, mushroom, or branched, with a continuum of intermediate morphologies. They typically terminate in a bulb shape, linked to the dendritic shaft by a restriction. Spine remodeling is though to be involved in synaptic plasticity. [GOC:nln]
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]
synaptic membrane	cellular component	A specialized area of membrane on either the presynaptic or the postsynaptic side of a synapse, the junction between a nerve fiber of one neuron and another neuron or muscle fiber or glial cell. [GOC:BHF, PMID:20410104]
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
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 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]

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 35 target(s):

Target	Category	Definition
startle response	biological process	An action or movement due to the application of a sudden unexpected stimulus. [GOC:dph]
response to amphetamine	biological process	Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an amphetamine stimulus. Amphetamines consist of a group of compounds related to alpha-methylphenethylamine. [GOC:dph, GOC:ef]
glutamate receptor signaling pathway	biological process	The series of molecular signals initiated by the binding of glutamate to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:mah, GOC:signaling, PMID:9131252]
chemical synaptic transmission	biological process	The vesicular release of classical neurotransmitter molecules from a presynapse, across a chemical synapse, the subsequent activation of neurotransmitter 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:jl, MeSH:D009435]
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]
learning or memory	biological process	The acquisition and processing of information and/or the storage and retrieval of this information over time. [GOC:jid, PMID:8938125]
memory	biological process	The activities involved in the mental information processing system that receives (registers), modifies, stores, and retrieves informational stimuli. The main stages involved in the formation and retrieval of memory are encoding (processing of received information by acquisition), storage (building a permanent record of received information as a result of consolidation) and retrieval (calling back the stored information and use it in a suitable way to execute a given task). [GOC:curators, ISBN:0582227089]
visual learning	biological process	Any process in an organism in which a change in behavior of an individual occurs in response to repeated exposure to a visual cue. [GOC:jid, ISBN:0582227089]
response to xenobiotic stimulus	biological process	Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus from a xenobiotic, a compound foreign to the organim exposed to it. It may be synthesized by another organism (like ampicilin) or it can be a synthetic chemical. [GOC:jl, GOC:krc]
response to wounding	biological process	Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus indicating damage to the organism. [GOC:go_curators]
sensory perception of pain	biological process	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. Pain is medically defined as the physical sensation of discomfort or distress caused by injury or illness, so can hence be described as a harmful stimulus which signals current (or impending) tissue damage. Pain may come from extremes of temperature, mechanical damage, electricity or from noxious chemical substances. This is a neurological process. [GOC:curators]
calcium-mediated signaling	biological process	Any intracellular signal transduction in which the signal is passed on within the cell via calcium ions. [GOC:signaling]
neurogenesis	biological process	Generation of cells within the nervous system. [GO_REF:0000021, GOC:cls, GOC:curators, GOC:dgh, GOC:dph, GOC:jid]
protein catabolic process	biological process	The chemical reactions and pathways resulting in the breakdown of a protein by the destruction of the native, active configuration, with or without the hydrolysis of peptide bonds. [GOC:mah]
sleep	biological process	Any process in which an organism enters and maintains a periodic, readily reversible state of reduced awareness and metabolic activity. Usually accompanied by physical relaxation, the onset of sleep in humans and other mammals is marked by a change in the electrical activity of the brain. [ISBN:0192800981]
directional locomotion	biological process	Self-propelled movement of a cell or organism from one location to another along an axis. [GOC:mtg_MIT_16mar07]
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]
negative regulation of protein catabolic process	biological process	Any process that stops, prevents or reduces the frequency, rate or extent of protein catabolic process. [GO_REF:0000058, GOC:kmv, GOC:obol, GOC:TermGenie, PMID:24785082]
dopamine metabolic process	biological process	The chemical reactions and pathways involving dopamine, a catecholamine neurotransmitter and a metabolic precursor of noradrenaline and adrenaline. [GOC:jl, ISBN:0198506732]
serotonin metabolic process	biological process	The chemical reactions and pathways involving serotonin (5-hydroxytryptamine), a monoamine neurotransmitter occurring in the peripheral and central nervous systems, also having hormonal properties. [GOC:jl, ISBN:0198506732]
positive regulation of apoptotic process	biological process	Any process that activates or increases the frequency, rate or extent of cell death by apoptotic process. [GOC:jl, GOC:mtg_apoptosis]
response to ethanol	biological process	Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an ethanol stimulus. [GOC:go_curators]
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]
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]
activation of cysteine-type endopeptidase activity	biological process	Any process that initiates the activity of the inactive enzyme cysteine-type endopeptidase. [GOC:mtg_apoptosis, PMID:21726810]
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]
protein localization to postsynaptic membrane	biological process	A process in which a protein is transported to, or maintained in, a location within a postsynaptic membrane. [GO_REF:0000087, GOC:kmv, GOC:TermGenie, PMID:9753322]
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]
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]