Proteins > Glutamate receptor ionotropic, NMDA 3B
Page last updated: 2024-08-07 15:26:06
Glutamate receptor ionotropic, NMDA 3B
A glutamate receptor ionotropic, NMDA 3B that is encoded in the genome of human. [PRO:DNx, UniProtKB:O60391]
Synonyms
GluN3B;
N-methyl-D-aspartate receptor subtype 3B;
NMDAR3B;
NR3B
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 6 target(s):
| Target | Category | Definition |
|---|
| monoatomic cation channel activity | molecular function | Enables the energy-independent passage of monoatomic cations across a lipid bilayer down a concentration gradient. [GOC:def, GOC:dph, GOC:mtg_transport, GOC:pr, ISBN:0815340729] |
| glycine binding | molecular function | Binding to glycine, aminoethanoic acid. [GOC:ai] |
| neurotransmitter receptor activity | molecular function | Combining with a neurotransmitter and transmitting the signal to initiate a change in cell activity. [GOC:jl, GOC:signaling] |
| 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] |
| 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] |
Located In
This protein is located in 1 target(s):
| Target | Category | Definition |
|---|
| 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] |
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 8 target(s):
| Target | Category | Definition |
|---|
| 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] |
| protein insertion into membrane | biological process | The process that results in the incorporation of a protein into a biological membrane. Incorporation in this context means having some part or covalently attached group that is inserted into the the hydrophobic region of one or both bilayers. [GOC:ai] |
| regulation of calcium ion transport | biological process | Any process that modulates the frequency, rate or extent of the directed movement of calcium ions into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. [GOC:ai] |
| regulation of postsynaptic membrane potential | biological process | Any process that modulates the potential difference across a post-synaptic membrane. [GOC:dph, GOC:ef] |
| 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] |
| regulation of presynaptic membrane potential | biological process | Any process that modulates the potential difference across a presynaptic membrane. [GOC:dph, GOC:ef] |
| 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] |
| 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] |