Proteins > Metabotropic glutamate receptor 2
Page last updated: 2024-08-07 17:07:14
Metabotropic glutamate receptor 2
A metabotropic glutamate receptor 2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q14416]
Synonyms
mGluR2
Research
Bioassay Publications (41)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 11 (26.83) | 18.2507 |
| 2000's | 19 (46.34) | 29.6817 |
| 2010's | 11 (26.83) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (44)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| alpha-methyl-4-carboxyphenylglycine | Homo sapiens (human) | IC50 | 195.0000 | 2 | 2 |
| alpha-methyl-4-carboxyphenylglycine | Homo sapiens (human) | Ki | 195.5000 | 1 | 2 |
| ibotenic acid | Homo sapiens (human) | Ki | 110.0000 | 1 | 1 |
| 4-carboxy-3-hydroxyphenylglycine | Homo sapiens (human) | IC50 | 48.0000 | 1 | 1 |
| 4-carboxy-3-hydroxyphenylglycine | Homo sapiens (human) | Ki | 20.0000 | 1 | 1 |
| 1-aminoindan-1,5-dicarboxylic acid | Homo sapiens (human) | Ki | 1,000.0000 | 1 | 1 |
| 4-carboxyphenylglycine | Homo sapiens (human) | IC50 | 577.0000 | 1 | 1 |
| glutamic acid | Homo sapiens (human) | Ki | 7.6500 | 4 | 4 |
| quisqualic acid | Homo sapiens (human) | Ki | 556.5000 | 2 | 2 |
| L-2-aminoadipic acid | Homo sapiens (human) | Ki | 35.0000 | 1 | 1 |
| 1-amino-1,3-dicarboxycyclopentane | Homo sapiens (human) | Ki | 5.0000 | 1 | 1 |
| homocysteic acid | Homo sapiens (human) | Ki | 300.0000 | 1 | 1 |
| 2-amino-4-phosphonobutyric acid | Homo sapiens (human) | Ki | 709.6667 | 3 | 3 |
| eglumetad | Homo sapiens (human) | IC50 | 0.0063 | 2 | 2 |
| eglumetad | Homo sapiens (human) | Ki | 0.0595 | 8 | 8 |
| 3,5-dihydroxyphenylglycine | Homo sapiens (human) | Ki | 1,000.0000 | 2 | 2 |
| alpha-methyl-4-carboxyphenylglycine | Homo sapiens (human) | IC50 | 4.3000 | 1 | 1 |
| 6-methyl-2-(phenylethynyl)pyridine | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| 4-methylglutamic acid, threo-(l)-isomer | Homo sapiens (human) | Ki | 2.0000 | 1 | 1 |
| sib 1757 | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| l-2-(carboxypropyl)glycine | Homo sapiens (human) | Ki | 0.4900 | 1 | 1 |
| 2-(2,3-dicarboxycyclopropyl)glycine | Homo sapiens (human) | Ki | 0.1100 | 1 | 1 |
| 2r,4r-4-aminopyrrolidine-2,4-dicarboxylate | Homo sapiens (human) | Ki | 0.4500 | 1 | 1 |
| upf 596 | Homo sapiens (human) | IC50 | 300.0000 | 1 | 1 |
| upf 596 | Homo sapiens (human) | Ki | 300.0000 | 1 | 1 |
| sib 1893 | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| ly 341495 | Homo sapiens (human) | IC50 | 0.0469 | 6 | 6 |
| ly 341495 | Homo sapiens (human) | Ki | 0.0127 | 2 | 2 |
| n-(4-(2-methoxyphenoxy)phenyl)-n-(2,2,2-trifluoroethylsulfonyl)pyrid-3-ylmethylamine | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| ly 404039 | Homo sapiens (human) | Ki | 0.1490 | 1 | 1 |
| biphenyl-indanone a | Homo sapiens (human) | Ki | 0.0603 | 1 | 1 |
| ly 389795 | Homo sapiens (human) | Ki | 0.0039 | 1 | 1 |
| ly 379268 | Homo sapiens (human) | Ki | 0.4135 | 3 | 5 |
| a 794282 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| sp 203 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| jnj-40411813 | Homo sapiens (human) | IC50 | 0.0680 | 1 | 1 |
| jnj-40411813 | Homo sapiens (human) | Ki | 0.1800 | 1 | 1 |
| ml289 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| ibotenic acid | Homo sapiens (human) | EC50 | 110.0000 | 1 | 1 |
| aspartic acid | Homo sapiens (human) | EC50 | 1,000.0000 | 1 | 1 |
| d-glutamate | Homo sapiens (human) | EC50 | 1,000.0000 | 1 | 1 |
| glutamic acid | Homo sapiens (human) | EC50 | 7.3849 | 12 | 13 |
| quisqualic acid | Homo sapiens (human) | EC50 | 1,000.0000 | 1 | 1 |
| 1-amino-1,3-dicarboxycyclopentane, (trans)-isomer | Homo sapiens (human) | EC50 | 110.0000 | 1 | 1 |
| d-aspartic acid | Homo sapiens (human) | EC50 | 1,000.0000 | 1 | 1 |
| L-2-aminoadipic acid | Homo sapiens (human) | EC50 | 35.0000 | 1 | 1 |
| alpha-aminopimelic acid | Homo sapiens (human) | EC50 | 1,000.0000 | 1 | 1 |
| 1-amino-1,3-dicarboxycyclopentane | Homo sapiens (human) | EC50 | 10.7000 | 3 | 3 |
| alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid | Homo sapiens (human) | EC50 | 1,000.0000 | 1 | 1 |
| alpha-amino-3-(hydroxy)-5-methyl-4-isoxazoleacetic acid | Homo sapiens (human) | EC50 | 1,000.0000 | 2 | 2 |
| 2-amino-4-phosphonobutyric acid | Homo sapiens (human) | EC50 | 1,000.0000 | 3 | 3 |
| eglumetad | Homo sapiens (human) | EC50 | 0.0113 | 8 | 8 |
| l-2-(carboxypropyl)glycine | Homo sapiens (human) | EC50 | 0.3800 | 1 | 1 |
| upf 596 | Homo sapiens (human) | EC50 | 300.0000 | 1 | 1 |
| 4-carboxy-3-hydroxyphenylglycine | Homo sapiens (human) | EC50 | 48.0000 | 1 | 1 |
| 1-amino-1,3-dicarboxycyclopentane, cis-(1s,3s)-isomer | Homo sapiens (human) | EC50 | 13.0000 | 2 | 2 |
| ampa, (r)-isomer | Homo sapiens (human) | EC50 | 1,000.0000 | 1 | 1 |
| n-(4-(2-methoxyphenoxy)phenyl)-n-(2,2,2-trifluoroethylsulfonyl)pyrid-3-ylmethylamine | Homo sapiens (human) | EC50 | 1.2233 | 3 | 3 |
| ly 404039 | Homo sapiens (human) | EC50 | 0.0234 | 1 | 1 |
| mgs 0028 | Homo sapiens (human) | EC50 | 0.0006 | 1 | 1 |
| biphenyl-indanone a | Homo sapiens (human) | EC50 | 0.0604 | 2 | 2 |
| biphenyl-indanone a | Homo sapiens (human) | Kd | 0.1900 | 1 | 1 |
| ly 379268 | Homo sapiens (human) | EC50 | 0.0027 | 3 | 3 |
| jnj-40411813 | Homo sapiens (human) | EC50 | 0.9168 | 9 | 9 |
Drugs with Other Measurements
Ligands for glutamate receptors: design and therapeutic prospects.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
Synthesis and pharmacological characterization of all sixteen stereoisomers of 2-(2'-carboxy-3'-phenylcyclopropyl)glycine. Focus on (2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-phenylcyclopropyl)glycine, a novel and selective group II metabotropic glutamate receptorJournal of medicinal chemistry, , May-24, Volume: 39, Issue:11, 1996
1-Aminoindan-1,5-dicarboxylic acid: a novel antagonist at phospholipase C-linked metabotropic glutamate receptors.Journal of medicinal chemistry, , Sep-15, Volume: 38, Issue:19, 1995
Ligands for glutamate receptors: design and therapeutic prospects.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
Synthesis and pharmacology of N-alkylated derivatives of the excitotoxin ibotenic acid.Bioorganic & medicinal chemistry letters, , Jun-16, Volume: 8, Issue:12, 1998
Ligands for glutamate receptors: design and therapeutic prospects.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
1-Aminoindan-1,5-dicarboxylic acid: a novel antagonist at phospholipase C-linked metabotropic glutamate receptors.Journal of medicinal chemistry, , Sep-15, Volume: 38, Issue:19, 1995
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
New positive allosteric modulators of the metabotropic glutamate receptor 2 (mGluR2): identification and synthesis of N-propyl-8-chloro-6-substituted isoquinolones.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 21, Issue:3, 2011
Design, synthesis and biological evaluation of novel bicyclo[1.1.1]pentane-based omega-acidic amino acids as glutamate receptors ligands.Bioorganic & medicinal chemistry, , Jan-01, Volume: 17, Issue:1, 2009
Synthesis, molecular modeling studies, and preliminary pharmacological characterization of all possible 2-(2'-sulfonocyclopropyl)glycine stereoisomers as conformationally constrained L-homocysteic acid analogs.Journal of medicinal chemistry, , Sep-20, Volume: 50, Issue:19, 2007
Synthesis and preliminary pharmacological evaluation of the four stereoisomers of (2S)-2-(2'-phosphono-3'-phenylcyclopropyl)glycine, the first class of 3'-substituted trans C1'-2'-2-(2'-phosphonocyclopropyl)glycines.Bioorganic & medicinal chemistry, , May-01, Volume: 15, Issue:9, 2007
Synthesis and preliminary biological evaluation of (2S,1'R,2'S)- and (2S,1'S,2'R)-2-(2'-phosphonocyclopropyl)glycines, two novel conformationally constrained l-AP4 analogues.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 16, Issue:1, 2006
(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
Common and selective molecular determinants involved in metabotopic glutamate receptor agonist activity.Journal of medicinal chemistry, , Jul-18, Volume: 45, Issue:15, 2002
Design, synthesis and preliminary evaluation of novel 3'-substituted carboxycyclopropylglycines as antagonists at group 2 metabotropic glutamate receptors.Bioorganic & medicinal chemistry letters, , Dec-17, Volume: 11, Issue:24, 2001
Ligands for glutamate receptors: design and therapeutic prospects.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
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
A new highly selective metabotropic excitatory amino acid agonist: 2-amino-4-(3-hydroxy-5-methylisoxazol-4-yl)butyric acid.Journal of medicinal chemistry, , Aug-02, Volume: 39, Issue:16, 1996
Metabotropic glutamate receptors: novel targets for drug development.Journal of medicinal chemistry, , Apr-28, Volume: 38, Issue:9, 1995
Common and selective molecular determinants involved in metabotopic glutamate receptor agonist activity.Journal of medicinal chemistry, , Jul-18, Volume: 45, Issue:15, 2002
Ligands for glutamate receptors: design and therapeutic prospects.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
Metabotropic glutamate receptors: novel targets for drug development.Journal of medicinal chemistry, , Apr-28, Volume: 38, Issue:9, 1995
Ligands for glutamate receptors: design and therapeutic prospects.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
A new highly selective metabotropic excitatory amino acid agonist: 2-amino-4-(3-hydroxy-5-methylisoxazol-4-yl)butyric acid.Journal of medicinal chemistry, , Aug-02, Volume: 39, Issue:16, 1996
(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 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
Synthesis and pharmacological characterization of aminocyclopentanetricarboxylic acids: new tools to discriminate between metabotropic glutamate receptor subtypes.Journal of medicinal chemistry, , Sep-12, Volume: 40, Issue:19, 1997
Metabotropic glutamate receptors: novel targets for drug development.Journal of medicinal chemistry, , Apr-28, Volume: 38, Issue:9, 1995
Synthesis and pharmacology of N-alkylated derivatives of the excitotoxin ibotenic acid.Bioorganic & medicinal chemistry letters, , Jun-16, Volume: 8, Issue:12, 1998
A new highly selective metabotropic excitatory amino acid agonist: 2-amino-4-(3-hydroxy-5-methylisoxazol-4-yl)butyric acid.Journal of medicinal chemistry, , Aug-02, Volume: 39, Issue:16, 1996
Design, synthesis and biological evaluation of novel bicyclo[1.1.1]pentane-based omega-acidic amino acids as glutamate receptors ligands.Bioorganic & medicinal chemistry, , Jan-01, Volume: 17, Issue:1, 2009
Synthesis and preliminary pharmacological evaluation of the four stereoisomers of (2S)-2-(2'-phosphono-3'-phenylcyclopropyl)glycine, the first class of 3'-substituted trans C1'-2'-2-(2'-phosphonocyclopropyl)glycines.Bioorganic & medicinal chemistry, , May-01, Volume: 15, Issue:9, 2007
Synthesis and preliminary biological evaluation of (2S,1'R,2'S)- and (2S,1'S,2'R)-2-(2'-phosphonocyclopropyl)glycines, two novel conformationally constrained l-AP4 analogues.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 16, Issue:1, 2006
Common and selective molecular determinants involved in metabotopic glutamate receptor agonist activity.Journal of medicinal chemistry, , Jul-18, Volume: 45, Issue:15, 2002
Ligands for glutamate receptors: design and therapeutic prospects.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
Metabotropic glutamate receptors: novel targets for drug development.Journal of medicinal chemistry, , Apr-28, Volume: 38, Issue:9, 1995
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
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
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
(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
Common and selective molecular determinants involved in metabotopic glutamate receptor agonist activity.Journal of medicinal chemistry, , Jul-18, Volume: 45, Issue:15, 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 metabotropic glutamate receptor activity of a 2-aminobicyclo[3.2.0]heptane-2,5-dicarboxylic acid, a molecule possessing an extended glutamate conformation.Bioorganic & medicinal chemistry letters, , Apr-21, Volume: 8, Issue:8, 1998
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
Common and selective molecular determinants involved in metabotopic glutamate receptor agonist activity.Journal of medicinal chemistry, , Jul-18, Volume: 45, Issue:15, 2002
Ligands for glutamate receptors: design and therapeutic prospects.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
(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
Metabotropic glutamate receptors: novel targets for drug development.Journal of medicinal chemistry, , Apr-28, Volume: 38, Issue:9, 1995
(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
Common and selective molecular determinants involved in metabotopic glutamate receptor agonist activity.Journal of medicinal chemistry, , Jul-18, Volume: 45, Issue:15, 2002
Ligands for glutamate receptors: design and therapeutic prospects.Journal of medicinal chemistry, , Jul-13, Volume: 43, Issue:14, 2000
(S)-(+)-2-(3'-carboxybicyclo[1.1.1]pentyl)-glycine, a structurally new group I metabotropic glutamate receptor antagonist.Journal of medicinal chemistry, , Jul-19, Volume: 39, Issue:15, 1996
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
Synthesis and pharmacological characterization of aminocyclopentanetricarboxylic acids: new tools to discriminate between metabotropic glutamate receptor subtypes.Journal of medicinal chemistry, , Sep-12, Volume: 40, Issue:19, 1997
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
Synthesis, in vitro pharmacology, and pharmacokinetic profiles of 2-[1-amino-1-carboxy-2-(9H-xanthen-9-yl)-ethyl]-1-fluorocyclopropanecarboxylic acid and its 6-heptyl ester, a potent mGluR2 antagonist.Bioorganic & medicinal chemistry, , Apr-15, Volume: 16, Issue:8, 2008
Design, synthesis and preliminary evaluation of novel 3'-substituted carboxycyclopropylglycines as antagonists at group 2 metabotropic glutamate receptors.Bioorganic & medicinal chemistry letters, , Dec-17, Volume: 11, Issue:24, 2001
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
Pyrimidine methyl anilines: selective potentiators for the metabotropic glutamate 2 receptor.Bioorganic & medicinal chemistry letters, , Oct-18, Volume: 14, Issue:20, 2004
Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 1: Identification and synthesis of phenyl-tetrazolyl acetophenones.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 14, Issue:21, 2004
Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 2: 4-thiopyridyl acetophenones as non-tetrazole containing mGlu2 receptor potentiators.Bioorganic & medicinal chemistry letters, , Dec-06, Volume: 14, Issue:23, 2004
Discovery of allosteric potentiators for the metabotropic glutamate 2 receptor: synthesis and subtype selectivity of N-(4-(2-methoxyphenoxy)phenyl)-N-(2,2,2- trifluoroethylsulfonyl)pyrid-3-ylmethylamine.Journal of medicinal chemistry, , Jul-17, Volume: 46, Issue:15, 2003
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
Discovery and Kinetic Profiling of 7-Aryl-1,2,4-triazolo[4,3-a]pyridines: Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 2.Journal of medicinal chemistry, , 08-10, Volume: 60, Issue:15, 2017
Scaffold hopping from pyridones to imidazo[1,2-a]pyridines. New positive allosteric modulators of metabotropic glutamate 2 receptor.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 20, Issue:1, 2010
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
Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).Journal of medicinal chemistry, , 09-22, Volume: 59, Issue:18, 2016
Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor.Journal of medicinal chemistry, , Aug-14, Volume: 57, Issue:15, 2014
Enables
This protein enables 6 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] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| 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 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] |
| 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] |
| 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] |
| 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] |
| 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 16 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] |
| glutamate secretion | biological process | The controlled release of glutamate by a cell. The glutamate is the most abundant excitatory neurotransmitter in the nervous system. [GOC:ef] |
| regulation of glutamate secretion | biological process | Any process that modulates the frequency, rate or extent of the controlled release of glutamate. [GOC:ef] |
| regulation of dopamine secretion | biological process | Any process that modulates the frequency, rate or extent of the regulated release of dopamine. [GOC:ef] |
| behavioral response to nicotine | biological process | Any process that results in a change in the behavior of an organism as a result of a nicotine stimulus. [GOC:bf, ISBN:0198506732] |
| response to cocaine | 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 cocaine stimulus. Cocaine is a crystalline alkaloid obtained from the leaves of the coca plant. [GOC:ef, GOC:jl] |
| positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction | biological process | Any process that activates or increases the frequency, rate or extent of phosphatidylinositol 3-kinase/protein kinase B signal transduction. [GOC:ai] |
| long-term synaptic depression | biological process | A process that modulates synaptic plasticity such that synapses are changed resulting in the decrease in the rate, or frequency of synaptic transmission at the synapse. [GOC:dgh, GOC:dph] |
| intracellular glutamate homeostasis | biological process | A homeostatic process involved in the maintenance of a steady state level of glutamate within a cell. [GOC:tb] |
| presynaptic modulation of chemical synaptic transmission | biological process | Any process, acting in the presynapse that results in modulation of chemical synaptic transmission. [GOC:dos] |
| regulation of response to drug | biological process | Any process that modulates the frequency, rate or extent of response to drug. [GOC:obol] |
| 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] |
| 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] |