Proteins > Metabotropic glutamate receptor 3
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Metabotropic glutamate receptor 3
A metabotropic glutamate receptor 3 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q14832]
Synonyms
mGluR3
Research
Bioassay Publications (15)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 4 (26.67) | 18.2507 |
| 2000's | 5 (33.33) | 29.6817 |
| 2010's | 6 (40.00) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (18)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Drugs with Other Measurements
Synthesis and Pharmacological Characterization of C4-(Thiotriazolyl)-substituted-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylates. Identification of (1R,2S,4R,5R,6R)-2-Amino-4-(1H-1,2,4-triazol-3-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY2812Journal of medicinal chemistry, , Sep-24, Volume: 58, Issue:18, 2015
(2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-methylcyclopropyl) glycine is a potent and selective metabotropic group 2 receptor agonist with anxiolytic properties.Journal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
Ligands for glutamate receptors: design and therapeutic prospects.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
1-amino-APDC, a partial agonist of group II metabotropic glutamate receptors with neuroprotective properties.Bioorganic & medicinal chemistry letters, , Jun-21, Volume: 9, Issue:12, 1999
(2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-methylcyclopropyl) glycine is a potent and selective metabotropic group 2 receptor agonist with anxiolytic properties.Journal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
1-amino-APDC, a partial agonist of group II metabotropic glutamate receptors with neuroprotective properties.Bioorganic & medicinal chemistry letters, , Jun-21, Volume: 9, Issue:12, 1999
Synthesis and Pharmacological Characterization of C4Journal of medicinal chemistry, , 03-22, Volume: 61, Issue:6, 2018
Discovery of (1S,2R,3S,4S,5R,6R)-2-Amino-3-[(3,4-difluorophenyl)sulfanylmethyl]-4-hydroxy-bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid Hydrochloride (LY3020371·HCl): A Potent, Metabotropic Glutamate 2/3 Receptor Antagonist with Antidepressant-Like Activity.Journal of medicinal chemistry, , 12-22, Volume: 59, Issue:24, 2016
Synthesis and Pharmacological Characterization of C4-(Thiotriazolyl)-substituted-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylates. Identification of (1R,2S,4R,5R,6R)-2-Amino-4-(1H-1,2,4-triazol-3-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY2812Journal of medicinal chemistry, , Sep-24, Volume: 58, Issue:18, 2015
Synthesis and pharmacological characterization of 4-substituted-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylates: identification of new potent and selective metabotropic glutamate 2/3 receptor agonists.Journal of medicinal chemistry, , Jun-13, Volume: 56, Issue:11, 2013
Synthesis and metabotropic glutamate receptor activity of S-oxidized variants of (-)-4-amino-2-thiabicyclo-[3.1.0]hexane-4,6-dicarboxylate: identification of potent, selective, and orally bioavailable agonists for mGlu2/3 receptors.Journal of medicinal chemistry, , Jan-25, Volume: 50, Issue:2, 2007
Dipeptides as effective prodrugs of the unnatural amino acid (+)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY354740), a selective group II metabotropic glutamate receptor agonist.Journal of medicinal chemistry, , Aug-11, Volume: 48, Issue:16, 2005
Methyl substitution of 2-aminobicyclo[3.1.0]hexane 2,6-dicarboxylate (LY354740) determines functional activity at metabotropic glutamate receptors: identification of a subtype selective mGlu2 receptor agonist.Journal of medicinal chemistry, , May-19, Volume: 48, Issue:10, 2005
(2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-methylcyclopropyl) glycine is a potent and selective metabotropic group 2 receptor agonist with anxiolytic properties.Journal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
Ligands for glutamate receptors: design and therapeutic prospects.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
Synthesis, pharmacological characterization, and molecular modeling of heterobicyclic amino acids related to (+)-2-aminobicyclo[3.1.0] hexane-2,6-dicarboxylic acid (LY354740): identification of two new potent, selective, and systemically active agonists fJournal of medicinal chemistry, , Mar-25, Volume: 42, Issue:6, 1999
Synthesis and biology of the conformationally restricted ACPD analogue, 2-aminobicyclo[2.1.1]hexane-2,5-dicarboxylic acid-I, a potent mGluR agonist.Journal of medicinal chemistry, , May-07, Volume: 41, Issue:10, 1998
(2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-methylcyclopropyl) glycine is a potent and selective metabotropic group 2 receptor agonist with anxiolytic properties.Journal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
Ligands for glutamate receptors: design and therapeutic prospects.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
Ligands for glutamate receptors: design and therapeutic prospects.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
1-amino-APDC, a partial agonist of group II metabotropic glutamate receptors with neuroprotective properties.Bioorganic & medicinal chemistry letters, , Jun-21, Volume: 9, Issue:12, 1999
Discovery of (1S,2R,3S,4S,5R,6R)-2-Amino-3-[(3,4-difluorophenyl)sulfanylmethyl]-4-hydroxy-bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid Hydrochloride (LY3020371·HCl): A Potent, Metabotropic Glutamate 2/3 Receptor Antagonist with Antidepressant-Like Activity.Journal of medicinal chemistry, , 12-22, Volume: 59, Issue:24, 2016
Radiosynthesis of PET radiotracer as a prodrug for imaging group II metabotropic glutamate receptors in vivo.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 22, Issue:5, 2012
Ligands for glutamate receptors: design and therapeutic prospects.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
2-substituted (2SR)-2-amino-2-((1SR,2SR)-2-carboxycycloprop-1-yl)glycines as potent and selective antagonists of group II metabotropic glutamate receptors. 2. Effects of aromatic substitution, pharmacological characterization, and bioavailability.Journal of medicinal chemistry, , Jan-29, Volume: 41, Issue:3, 1998
Radiosynthesis of PET radiotracer as a prodrug for imaging group II metabotropic glutamate receptors in vivo.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 22, Issue:5, 2012
(2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-methylcyclopropyl) glycine is a potent and selective metabotropic group 2 receptor agonist with anxiolytic properties.Journal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
Radiosynthesis of PET radiotracer as a prodrug for imaging group II metabotropic glutamate receptors in vivo.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 22, Issue:5, 2012
Synthesis and metabotropic glutamate receptor activity of S-oxidized variants of (-)-4-amino-2-thiabicyclo-[3.1.0]hexane-4,6-dicarboxylate: identification of potent, selective, and orally bioavailable agonists for mGlu2/3 receptors.Journal of medicinal chemistry, , Jan-25, Volume: 50, Issue:2, 2007
(2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-methylcyclopropyl) glycine is a potent and selective metabotropic group 2 receptor agonist with anxiolytic properties.Journal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
Ligands for glutamate receptors: design and therapeutic prospects.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
Synthesis, pharmacological characterization, and molecular modeling of heterobicyclic amino acids related to (+)-2-aminobicyclo[3.1.0] hexane-2,6-dicarboxylic acid (LY354740): identification of two new potent, selective, and systemically active agonists fJournal of medicinal chemistry, , Mar-25, Volume: 42, Issue:6, 1999
Enables
This protein enables 5 target(s):
| Target | Category | Definition |
|---|
| G protein-coupled receptor activity | molecular function | Combining with an extracellular signal and transmitting the signal across the membrane by activating an associated G-protein; promotes the exchange of GDP for GTP on the alpha subunit of a heterotrimeric G-protein complex. [GOC:bf, http://www.iuphar-db.org, Wikipedia:GPCR] |
| calcium channel regulator activity | molecular function | Modulates the activity of a calcium channel. [GOC:mah] |
| 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] |
| scaffold protein binding | molecular function | Binding to a scaffold protein. Scaffold proteins are crucial regulators of many key signaling pathways. Although not strictly defined in function, they are known to interact and/or bind with multiple members of a signaling pathway, tethering them into complexes. [GOC:BHF, GOC:sjp, PMID:10433269, Wikipedia:Scaffold_protein] |
| group II metabotropic glutamate receptor activity | molecular function | A G protein-coupled receptor that is activated by trans-1-aminocyclopentane-1,3-dicarboxylic acid (t-ACPD) and inhibits adenylate cyclase activity. [GOC:dph] |
Located In
This protein is located in 8 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 | 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] |
| axon | cellular component | The long process of a neuron that conducts nerve impulses, usually away from the cell body to the terminals and varicosities, which are sites of storage and release of neurotransmitter. [GOC:nln, ISBN:0198506732] |
| 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] |
| astrocyte projection | cellular component | A prolongation or process extending from the soma of an astrocyte and wrapping around neurons. [NIF_Subcellular:sao1630537580] |
| glutamatergic synapse | cellular component | A synapse that uses glutamate as a neurotransmitter. [GOC:dos] |
Active In
This protein is active in 1 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] |
Involved In
This protein is involved in 7 target(s):
| Target | Category | Definition |
|---|
| negative regulation of adenylate cyclase activity | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of adenylate cyclase activity. [GOC:go_curators] |
| adenylate cyclase-inhibiting G protein-coupled glutamate receptor signaling pathway | biological process | An adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway initiated by glutamate binding to its receptor, and ending with the regulation of a downstream cellular process. [GOC:dph, GOC:mah, GOC:signaling, GOC:tb] |
| 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] |
| gene expression | biological process | The process in which a gene's sequence is converted into a mature gene product (protein or RNA). This includes the production of an RNA transcript and its processing, as well as translation and maturation for protein-coding genes. [GOC:txnOH-2018, PMID:25934543, PMID:31580950] |
| postsynaptic modulation of chemical synaptic transmission | biological process | Any process, acting in the postsynapse that results in modulation of chemical synaptic transmission. [GOC:dos] |
| regulation of synaptic transmission, glutamatergic | biological process | Any process that modulates 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] |
| G protein-coupled glutamate receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway initiated by glutamate binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process. [GOC:mah, GOC:signaling, PMID:9131252] |