Page last updated: 2024-08-07 16:43:50
Glutamate receptor 4
A glutamate receptor 4 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P48058]
Synonyms
GluR-4;
GluR4;
AMPA-selective glutamate receptor 4;
GluR-D;
Glutamate receptor ionotropic, AMPA 4;
GluA4
Research
Bioassay Publications (23)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 5 (21.74) | 18.2507 |
| 2000's | 13 (56.52) | 29.6817 |
| 2010's | 4 (17.39) | 24.3611 |
| 2020's | 1 (4.35) | 2.80 |
Compounds (55)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| aminolevulinic acid | Homo sapiens (human) | Ki | 790.0000 | 1 | 1 |
| 5-aminovaleric acid | Homo sapiens (human) | Ki | 17,400.0000 | 1 | 1 |
| alanylalanine | Homo sapiens (human) | Ki | 120.0000 | 1 | 1 |
| alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid | Homo sapiens (human) | IC50 | 0.1353 | 3 | 3 |
| alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid | Homo sapiens (human) | Ki | 0.0400 | 1 | 1 |
| kainic acid | Homo sapiens (human) | Ki | 1.7113 | 3 | 3 |
| glycylglycine | Homo sapiens (human) | Ki | 1,000.0000 | 1 | 1 |
| glutamic acid | Homo sapiens (human) | IC50 | 0.6130 | 1 | 1 |
| glutamic acid | Homo sapiens (human) | Ki | 0.8680 | 3 | 3 |
| selfotel | Homo sapiens (human) | IC50 | 0.9670 | 1 | 1 |
| leucyl-alanine | Homo sapiens (human) | Ki | 120.0000 | 1 | 1 |
| alanylproline | Homo sapiens (human) | Ki | 150.0000 | 1 | 1 |
| glycylleucine | Homo sapiens (human) | Ki | 160.0000 | 1 | 1 |
| alanyltyrosine | Homo sapiens (human) | Ki | 150.0000 | 1 | 1 |
| glycylsarcosine | Homo sapiens (human) | Ki | 830.0000 | 1 | 1 |
| glycylaspartic acid | Homo sapiens (human) | Ki | 350.0000 | 1 | 1 |
| histidinoalanine | Homo sapiens (human) | Ki | 480.0000 | 1 | 1 |
| argiotoxin-636 | Homo sapiens (human) | IC50 | 0.4300 | 1 | 1 |
| 2-amino-3-(3-(carboxymethoxy)-5-methylisoxazol-4-yl)propionic acid | Homo sapiens (human) | IC50 | 93.0000 | 2 | 2 |
| 5-fluorowillardiine | Homo sapiens (human) | Ki | 0.3050 | 1 | 1 |
| ly 293558 | Homo sapiens (human) | IC50 | 3.0750 | 2 | 2 |
| ly 293558 | Homo sapiens (human) | Ki | 50.2500 | 2 | 2 |
| alanylglutamic acid | Homo sapiens (human) | Ki | 320.0000 | 1 | 1 |
| prolyl-tyrosine | Homo sapiens (human) | Ki | 730.0000 | 1 | 1 |
| alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid | Homo sapiens (human) | Ki | 0.0975 | 2 | 2 |
| 5-bromowillardiine | Homo sapiens (human) | Ki | 0.4570 | 1 | 1 |
| prolylglutamic acid | Homo sapiens (human) | Ki | 20,000.0000 | 1 | 1 |
| cysteinylglycine | Homo sapiens (human) | Ki | 200.0000 | 1 | 1 |
| willardiine | Homo sapiens (human) | Ki | 8.8500 | 1 | 1 |
| aspartyl-aspartic acid | Homo sapiens (human) | Ki | 410.0000 | 1 | 1 |
| 4-bromohomoibotenic acid, (rs)-isomer | Homo sapiens (human) | Ki | 11.7000 | 1 | 1 |
| glycylproline | Homo sapiens (human) | Ki | 300.0000 | 1 | 1 |
| 2,3-dioxo-6-nitro-7-sulfamoylbenzo(f)quinoxaline | Homo sapiens (human) | IC50 | 1.1000 | 1 | 1 |
| 2,3-dioxo-6-nitro-7-sulfamoylbenzo(f)quinoxaline | Homo sapiens (human) | Ki | 0.6000 | 1 | 1 |
| 6-cyano-7-nitroquinoxaline-2,3-dione | Homo sapiens (human) | IC50 | 1.0200 | 3 | 3 |
| fg 9041 | Homo sapiens (human) | IC50 | 1.5100 | 3 | 3 |
| fg 9041 | Homo sapiens (human) | Ki | 0.3600 | 1 | 1 |
| seryl-proline | Homo sapiens (human) | Ki | 130.0000 | 1 | 1 |
| lofepramine hydrochloride | Homo sapiens (human) | Ki | 13.0947 | 3 | 3 |
| phenylalanylalanine | Homo sapiens (human) | Ki | 110.0000 | 1 | 1 |
| acetylalanylalanine | Homo sapiens (human) | Ki | 30,000.0000 | 1 | 1 |
| alpha-aspartylalanine | Homo sapiens (human) | Ki | 320.0000 | 1 | 1 |
| alanyltyrosine | Homo sapiens (human) | Ki | 90.0000 | 1 | 1 |
| prolylglycine | Homo sapiens (human) | Ki | 22,000.0000 | 1 | 1 |
| glutamylalanine | Homo sapiens (human) | Ki | 250.0000 | 1 | 1 |
| phenylalanylphenylalanine | Homo sapiens (human) | Ki | 110.0000 | 1 | 1 |
| phenylalanyl-valine | Homo sapiens (human) | Ki | 50.0000 | 1 | 1 |
| alanylglycine | Homo sapiens (human) | Ki | 140.0000 | 1 | 1 |
| valyltyrosine | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| phenylalanylproline | Homo sapiens (human) | Ki | 130.0000 | 1 | 1 |
| glycylhistidine | Homo sapiens (human) | Ki | 1,000.0000 | 1 | 1 |
| prolyl-serine | Homo sapiens (human) | Ki | 14,000.0000 | 1 | 1 |
| prolylvaline | Homo sapiens (human) | Ki | 60.0000 | 1 | 1 |
| tqx 173 | Homo sapiens (human) | IC50 | 6.9500 | 2 | 2 |
| tqx 173 | Homo sapiens (human) | Ki | 16.8200 | 2 | 2 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| aniracetam | Homo sapiens (human) | EC50 | 1,000.0000 | 1 | 1 |
| cyclothiazide | Homo sapiens (human) | EC50 | 3.8000 | 2 | 2 |
| glutamic acid | Homo sapiens (human) | EC50 | 9,952,675,009.4244 | 2 | 4 |
| bdp 12 | Homo sapiens (human) | EC50 | 718.6667 | 2 | 3 |
| (S)-ATPA | Homo sapiens (human) | EC50 | 7.6000 | 1 | 1 |
| ly 392098 | Homo sapiens (human) | EC50 | 4.4000 | 1 | 1 |
| ly 404187 | Homo sapiens (human) | EC50 | 0.4702 | 5 | 5 |
Drugs with Other Measurements
Design, synthesis, and pharmacology of a highly subtype-selective GluR1/2 agonist, (RS)-2-amino-3-(4-chloro-3-hydroxy-5-isoxazolyl)propionic acid (Cl-HIBO).Journal of medicinal chemistry, , May-22, Volume: 46, Issue:11, 2003
Heteroaryl analogues of AMPA. Synthesis and quantitative structure-activity relationships.Journal of medicinal chemistry, , Aug-29, Volume: 40, Issue:18, 1997
Novel class of amino acid antagonists at non-N-methyl-D-aspartic acid excitatory amino acid receptors. Synthesis, in vitro and in vivo pharmacology, and neuroprotection.Journal of medicinal chemistry, , Volume: 34, Issue:1, 1991
A novel class of AMPA receptor allosteric modulators. Part 1: design, synthesis, and SAR of 3-aryl-4-cyano-5-substituted-heteroaryl-2-carboxylic acid derivatives.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 16, Issue:19, 2006
Biarylpropylsulfonamides as novel, potent potentiators of 2-amino-3- (5-methyl-3-hydroxyisoxazol-4-yl)- propanoic acid (AMPA) receptors.Journal of medicinal chemistry, , Nov-16, Volume: 43, Issue:23, 2000
4-Alkylidenyl glutamic acids, potent and selective GluR5 agonists.Bioorganic & medicinal chemistry letters, , Aug-21, Volume: 10, Issue:16, 2000
4-Alkyl- and 4-cinnamylglutamic acid analogues are potent GluR5 kainate receptor agonists.Journal of medicinal chemistry, , May-18, Volume: 43, Issue:10, 2000
Synthesis of willardiine and 6-azawillardiine analogs: pharmacological characterization on cloned homomeric human AMPA and kainate receptor subtypes.Journal of medicinal chemistry, , Oct-24, Volume: 40, Issue:22, 1997
Use of the 4-Hydroxytriazole Moiety as a Bioisosteric Tool in the Development of Ionotropic Glutamate Receptor Ligands.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
Functional characterization of Tet-AMPA [tetrazolyl-2-amino-3-(3-hydroxy-5-methyl- 4-isoxazolyl)propionic acid] analogues at ionotropic glutamate receptors GluR1-GluR4. The molecular basis for the functional selectivity profile of 2-Bn-Tet-AMPA.Journal of medicinal chemistry, , Aug-23, Volume: 50, Issue:17, 2007
2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 2005
4-Alkylidenyl glutamic acids, potent and selective GluR5 agonists.Bioorganic & medicinal chemistry letters, , Aug-21, Volume: 10, Issue:16, 2000
4-Alkyl- and 4-cinnamylglutamic acid analogues are potent GluR5 kainate receptor agonists.Journal of medicinal chemistry, , May-18, Volume: 43, Issue:10, 2000
Synthesis of willardiine and 6-azawillardiine analogs: pharmacological characterization on cloned homomeric human AMPA and kainate receptor subtypes.Journal of medicinal chemistry, , Oct-24, Volume: 40, Issue:22, 1997
alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside.Journal of medicinal chemistry, , Aug-12, Volume: 53, Issue:15, 2010
Ethyl (3S,4aR,6S,8aR)-6-(4-ethoxycar- bonylimidazol-1-ylmethyl)decahydroiso-quinoline-3-carboxylic ester: a prodrug of a GluR5 kainate receptor antagonist active in two animal models of acute migraine.Journal of medicinal chemistry, , Sep-26, Volume: 45, Issue:20, 2002
(3SR,4aRS,6SR,8aRS)-6-(1H-tetrazol-5-yl)decahydroisoquinoline-3-carboxylic acid, a novel, competitive, systemically active NMDA and AMPA receptor antagonist.Journal of medicinal chemistry, , Dec-08, Volume: 38, Issue:25, 1995
(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
Positive allosteric modulators of the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor.Journal of medicinal chemistry, , Oct-28, Volume: 53, Issue:20, 2010
Biarylpropylsulfonamides as novel, potent potentiators of 2-amino-3- (5-methyl-3-hydroxyisoxazol-4-yl)- propanoic acid (AMPA) receptors.Journal of medicinal chemistry, , Nov-16, Volume: 43, Issue:23, 2000
Convergent synthesis and pharmacology of substituted tetrazolyl-2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid analogues.Journal of medicinal chemistry, , May-05, Volume: 48, Issue:9, 2005
Synthesis of willardiine and 6-azawillardiine analogs: pharmacological characterization on cloned homomeric human AMPA and kainate receptor subtypes.Journal of medicinal chemistry, , Oct-24, Volume: 40, Issue:22, 1997
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.Bioorganic & medicinal chemistry, , Feb-15, Volume: 18, Issue:4, 2010
Structure-activity relationship studies on N3-substituted willardiine derivatives acting as AMPA or kainate receptor antagonists.Journal of medicinal chemistry, , Apr-20, Volume: 49, Issue:8, 2006
Ethyl (3S,4aR,6S,8aR)-6-(4-ethoxycar- bonylimidazol-1-ylmethyl)decahydroiso-quinoline-3-carboxylic ester: a prodrug of a GluR5 kainate receptor antagonist active in two animal models of acute migraine.Journal of medicinal chemistry, , Sep-26, Volume: 45, Issue:20, 2002
Functionalized quinoxalinones as privileged structures with broad-ranging pharmacological activities.European journal of medicinal chemistry, , Feb-05, Volume: 229, 2022
(3SR,4aRS,6SR,8aRS)-6-(1H-tetrazol-5-yl)decahydroisoquinoline-3-carboxylic acid, a novel, competitive, systemically active NMDA and AMPA receptor antagonist.Journal of medicinal chemistry, , Dec-08, Volume: 38, Issue:25, 1995
Positive allosteric modulators of the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor.Journal of medicinal chemistry, , Oct-28, Volume: 53, Issue:20, 2010
A novel class of AMPA receptor allosteric modulators. Part 1: design, synthesis, and SAR of 3-aryl-4-cyano-5-substituted-heteroaryl-2-carboxylic acid derivatives.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 16, Issue:19, 2006
Design and synthesis of a novel series of 1,2-disubstituted cyclopentanes as small, potent potentiators of 2-amino-3-(3-hydroxy-5-methyl-isoxazol-4-yl)propanoic acid (AMPA) receptors.Journal of medicinal chemistry, , May-09, Volume: 45, Issue:10, 2002
Biarylpropylsulfonamides as novel, potent potentiators of 2-amino-3- (5-methyl-3-hydroxyisoxazol-4-yl)- propanoic acid (AMPA) receptors.Journal of medicinal chemistry, , Nov-16, Volume: 43, Issue:23, 2000
Enables
This protein enables 5 target(s):
| Target | Category | Definition |
|---|
| amyloid-beta binding | molecular function | Binding to an amyloid-beta peptide/protein. [GOC:hjd] |
| 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] |
| AMPA glutamate receptor activity | molecular function | An ionotropic glutamate receptor activity that exhibits fast gating by glutamate and acts by opening a cation channel permeable to sodium, potassium, and, in the absence of a GluR2 subunit, calcium. [GOC:mah, PMID:10049997, PMID:8804111] |
| 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 |
|---|
| 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] |
| 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] |
| endocytic vesicle membrane | cellular component | The lipid bilayer surrounding an endocytic vesicle. [GOC:mah] |
| 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] |
| 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] |
| extracellular vesicle | cellular component | Any vesicle that is part of the extracellular region. [GO_REF:0000064, GOC:pm, GOC:TermGenie, PMID:24769233] |
Active In
This protein is active in 3 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] |
| 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] |
Part Of
This protein is part of 1 target(s):
| Target | Category | Definition |
|---|
| AMPA 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. The AMPA receptors mediate fast synaptic transmission in the CNS and are composed of subunits GluR1-4, products from separate genes. These subunits have an extracellular N-terminus and an intracellular C-terminus. [GOC:ef] |
Involved In
This protein is involved in 8 target(s):
| Target | Category | Definition |
|---|
| 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] |
| monoatomic ion transmembrane transport | biological process | A process in which a monoatomic ion is transported across a membrane. Monatomic ions (also called simple ions) are ions consisting of exactly one atom. [GOC:mah] |
| negative regulation of smooth muscle cell apoptotic process | biological process | Any process that stops, prevents, or reduces the frequency, rate, or extent of smooth muscle cell apoptotic process. [GOC:BHF, GOC:mtg_apoptosis, GOC:rl] |
| 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 postsynaptic membrane potential | biological process | Any process that modulates the potential difference across a post-synaptic membrane. [GOC:dph, GOC:ef] |
| 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] |