Proteins > Glutamate receptor ionotropic, NMDA 3A
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Glutamate receptor ionotropic, NMDA 3A
A glutamate receptor ionotropic, NMDA 3A that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q8TCU5]
Synonyms
GluN3A;
N-methyl-D-aspartate receptor subtype 3A;
NMDAR3A;
NR3A;
NMDAR-L
Research
Bioassay Publications (25)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 7 (28.00) | 18.2507 |
| 2000's | 10 (40.00) | 29.6817 |
| 2010's | 4 (16.00) | 24.3611 |
| 2020's | 4 (16.00) | 2.80 |
Compounds (40)
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 |
| 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 |
| 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 |
| 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
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
Indole-2-carboxamides as novel NR2B selective NMDA receptor antagonists.Bioorganic & medicinal chemistry letters, , Nov-03, Volume: 13, Issue:21, 2003
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
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 |
|---|
| 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 channel activity | molecular function | Enables the facilitated diffusion of a calcium ion (by an energy-independent process) involving passage through a transmembrane aqueous pore or channel without evidence for a carrier-mediated mechanism. [GOC:mtg_transport, GOC:pr, ISBN:0815340729] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| glycine binding | molecular function | Binding to glycine, aminoethanoic acid. [GOC:ai] |
| identical protein binding | molecular function | Binding to an identical protein or proteins. [GOC:jl] |
| protein phosphatase 2A binding | molecular function | Binding to protein phosphatase 2A. [GOC:ai] |
| glutamate receptor activity | molecular function | Combining with glutamate and transmitting the signal from one side of the membrane to the other to initiate a change in cell activity. [GOC:ai, GOC:signaling] |
| 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 7 target(s):
| Target | Category | Definition |
|---|
| endoplasmic reticulum membrane | cellular component | The lipid bilayer surrounding the endoplasmic reticulum. [GOC:mah] |
| membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
| 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/] |
| neuronal cell body | cellular component | The portion of a neuron that includes the nucleus, but excludes cell projections such as axons and dendrites. [GOC:go_curators] |
| 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] |
| presynapse | cellular component | The part of a synapse that is part of the presynaptic cell. [GOC:dos] |
| 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 12 target(s):
| Target | Category | Definition |
|---|
| calcium ion transport | biological process | The directed movement of calcium (Ca) ions into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. [GOC:ai] |
| dendrite development | biological process | The process whose specific outcome is the progression of the dendrite over time, from its formation to the mature structure. [GOC:aruk, GOC:bc, GOC:jl, ISBN:0198506732, PMID:22683681] |
| 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] |
| rhythmic process | biological process | Any process pertinent to the generation and maintenance of rhythms in the physiology of an organism. [GOC:jid] |
| regulation of postsynaptic membrane potential | biological process | Any process that modulates the potential difference across a post-synaptic membrane. [GOC:dph, GOC:ef] |
| prepulse inhibition | biological process | The process in which a startle magnitude is reduced when the startling stimulus is preceded by a low-intensity prepulse. [GOC:dph, PMID:10341260] |
| negative regulation of dendritic spine development | biological process | Any process that decreases the rate, frequency, or extent of dendritic spine development, the process whose specific outcome is the progression of the dendritic spine over time, from its formation to the mature structure. [GOC:dph] |
| calcium ion transmembrane transport | biological process | A process in which a calcium ion is transported from one side of a membrane to the other by means of some agent such as a transporter or pore. [GOC:mah] |
| presynaptic modulation of chemical synaptic transmission | biological process | Any process, acting in the presynapse that results in modulation of chemical synaptic transmission. [GOC:dos] |
| 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] |
| 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] |
| modulation of chemical synaptic transmission | biological process | Any process that modulates the frequency or amplitude of synaptic transmission, the process of communication from a neuron to a target (neuron, muscle, or secretory cell) across a synapse. Amplitude, in this case, refers to the change in postsynaptic membrane potential due to a single instance of synaptic transmission. [GOC:ai] |