Glutamate receptor ionotropic, NMDA 1

A glutamate receptor ionotropic, NMDA 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q05586]

Synonyms

GluN1;
Glutamate [NMDA] receptor subunit zeta-1;
N-methyl-D-aspartate receptor subunit NR1;
NMD-R1

Research

Bioassay Publications (51)

Timeframe	Studies on this Protein(%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	7 (13.73)	18.2507
2000's	15 (29.41)	29.6817
2010's	22 (43.14)	24.3611
2020's	7 (13.73)	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	31.9167	6	6
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	0.2039	6	6
ifenprodil	Homo sapiens (human)	Ki	0.0100	2	2
ketamine	Homo sapiens (human)	IC50	3.7762	5	5
ketamine	Homo sapiens (human)	Ki	0.5720	5	5
kynurenic acid	Homo sapiens (human)	IC50	15.0000	1	1
memantine	Homo sapiens (human)	IC50	4.3212	10	10
memantine	Homo sapiens (human)	Ki	0.6933	3	3
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	0.5563	3	3
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
eliprodil	Homo sapiens (human)	Ki	0.0130	1	1
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	0.0060	4	4
philanthotoxin 343	Homo sapiens (human)	IC50	2.7390	1	1
dizocilpine	Homo sapiens (human)	IC50	0.0090	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	0.0185	2	2
cp 101,606	Homo sapiens (human)	Ki	0.0110	2	2
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	0.2730	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)	IC50	0.7730	2	2
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	0.0315	4	4
ro 25-6981	Homo sapiens (human)	Ki	0.0072	3	3
eaa-090	Homo sapiens (human)	IC50	3.8150	2	2
pd 174494	Homo sapiens (human)	IC50	0.0045	2	2
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	0.0160	2	2
tqx 173	Homo sapiens (human)	IC50	46.0000	1	1
(1rs,1's)-peaqx	Homo sapiens (human)	IC50	9.9593	3	3
etoxadrol	Homo sapiens (human)	Ki	0.0220	1	1
methoxydine	Homo sapiens (human)	IC50	9.9150	2	2
nitd 609	Homo sapiens (human)	IC50	10.0000	1	1
wms 1410	Homo sapiens (human)	IC50	0.0185	1	1
wms 1410	Homo sapiens (human)	Ki	0.0373	3	3

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	2	2
rosiglitazone	Homo sapiens (human)	EC50	0.0210	1	1
24-hydroxycholesterol	Homo sapiens (human)	EC50	0.2825	4	4
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 11 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]
calcium ion binding	molecular function	Binding to a calcium ion (Ca2+). [GOC:ai]
protein binding	molecular function	Binding to a protein. [GOC:go_curators]
calmodulin binding	molecular function	Binding to calmodulin, a calcium-binding protein with many roles, both in the calcium-bound and calcium-free states. [GOC:krc]
glycine binding	molecular function	Binding to glycine, aminoethanoic acid. [GOC:ai]
glutamate binding	molecular function	Binding to glutamate, the anion of 2-aminopentanedioic acid. [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]
protein-containing complex binding	molecular function	Binding to a macromolecular complex. [GOC:jl]
signaling receptor activity	molecular function	Receiving a signal and transmitting it in the cell to initiate a change in cell activity. A signal is a physical entity or change in state that is used to transfer information in order to trigger a response. [GOC:bf, GOC:signaling]
ligand-gated monoatomic ion channel activity	molecular function	Enables the transmembrane transfer of an ion by a channel that opens when a specific ligand has been bound by the channel complex or one of its constituent parts. [GOC:mtg_transport, ISBN:0815340729]

Located In

This protein is located in 15 target(s):

Target	Category	Definition
cytoplasm	cellular component	The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684]
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]
dendrite	cellular component	A neuron projection that has a short, tapering, morphology. Dendrites receive and integrate signals from other neurons or from sensory stimuli, and conduct nerve impulses towards the axon or the cell body. In most neurons, the impulse is conveyed from dendrites to axon via the cell body, but in some types of unipolar neuron, the impulse does not travel via the cell body. [GOC:aruk, GOC:bc, GOC:dos, GOC:mah, GOC:nln, ISBN:0198506732]
neuron projection	cellular component	A prolongation or process extending from a nerve cell, e.g. an axon or dendrite. [GOC:jl, http://www.cogsci.princeton.edu/~wn/]
synaptic cleft	cellular component	The narrow gap that separates the presynaptic and postsynaptic membranes, into which neurotransmitter is released. [GOC:jl, http://synapses.mcg.edu/anatomy/chemical/synapse.stm]
terminal bouton	cellular component	Terminal inflated portion of the axon, containing the specialized apparatus necessary to release neurotransmitters. The axon terminus is considered to be the whole region of thickening and the terminal bouton is a specialized region of it. [GOC:dph, GOC:mc, GOC:nln, PMID:10218156, PMID:8409967]
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]
synapse	cellular component	The junction between an axon of one neuron and a dendrite of another neuron, a muscle fiber or a glial cell. As the axon approaches the synapse it enlarges into a specialized structure, the presynaptic terminal bouton, which contains mitochondria and synaptic vesicles. At the tip of the terminal bouton is the presynaptic membrane; facing it, and separated from it by a minute cleft (the synaptic cleft) is a specialized area of membrane on the receiving cell, known as the postsynaptic membrane. In response to the arrival of nerve impulses, the presynaptic terminal bouton secretes molecules of neurotransmitters into the synaptic cleft. These diffuse across the cleft and transmit the signal to the postsynaptic membrane. [GOC:aruk, ISBN:0198506732, PMID:24619342, PMID:29383328, PMID:31998110]
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]
excitatory synapse	cellular component	A synapse in which an action potential in the presynaptic cell increases the probability of an action potential occurring in the postsynaptic cell. [GOC:dph, GOC:ef]
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]

Active In

This protein is active in 3 target(s):

Target	Category	Definition
synapse	cellular component	The junction between an axon of one neuron and a dendrite of another neuron, a muscle fiber or a glial cell. As the axon approaches the synapse it enlarges into a specialized structure, the presynaptic terminal bouton, which contains mitochondria and synaptic vesicles. At the tip of the terminal bouton is the presynaptic membrane; facing it, and separated from it by a minute cleft (the synaptic cleft) is a specialized area of membrane on the receiving cell, known as the postsynaptic membrane. In response to the arrival of nerve impulses, the presynaptic terminal bouton secretes molecules of neurotransmitters into the synaptic cleft. These diffuse across the cleft and transmit the signal to the postsynaptic membrane. [GOC:aruk, ISBN:0198506732, PMID:24619342, PMID:29383328, PMID:31998110]
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]
neuron projection	cellular component	A prolongation or process extending from a nerve cell, e.g. an axon or dendrite. [GOC:jl, http://www.cogsci.princeton.edu/~wn/]

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 24 target(s):

Target	Category	Definition
monoatomic cation transport	biological process	The directed movement of a monoatomic cation, into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. Monatomic cations (also called simple cations) are positively charged ions consisting of exactly one atom. [GOC:ai]
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]
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]
positive regulation of calcium ion transport into cytosol	biological process	Any process that increases the rate of the directed movement of calcium ions into the cytosol of a cell. The cytosol is that part of the cytoplasm that does not contain membranous or particulate subcellular components. [GOC:dph, GOC:tb]
propylene metabolic process	biological process	The chemical reactions and pathways involving propylene, an alkene produced by catalytic or thermal cracking of hydrocarbons or as a by-product of petroleum refining. It is used mainly in the preparation of alkylates for gasoline and in the production of polypropylene, acrylonitrile, propylene oxide and a number of other industrial chemicals. [GOC:jl]
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 membrane potential	biological process	Any process that modulates the establishment or extent of a membrane potential, the electric potential existing across any membrane arising from charges in the membrane itself and from the charges present in the media on either side of the membrane. [GOC:jl, GOC:mtg_cardio, GOC:tb, ISBN:0198506732]
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]
positive regulation of transcription by RNA polymerase II	biological process	Any process that activates or increases the frequency, rate or extent of transcription from an RNA polymerase II promoter. [GOC:go_curators, GOC:txnOH]
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]
protein heterotetramerization	biological process	The formation of a protein heterotetramer, a macromolecular structure consisting of four noncovalently associated subunits, of which not all are identical. [GOC:go_curators]
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 homeostasis	biological process	Any process involved in the maintenance of an internal steady state of calcium ions within an organism or cell. [GOC:ceb, GOC:jid, GOC:mah]
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]
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]
positive regulation of reactive oxygen species biosynthetic process	biological process	Any process that activates or increases the frequency, rate or extent of reactive oxygen species biosynthetic process. [GO_REF:0000058, GOC:bf, GOC:PARL, GOC:TermGenie, PMID:24252804]
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]
response to glycine	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 glycine stimulus. [GO_REF:0000071, GOC:TermGenie, PMID:18984164]
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]
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]