Target Information
Target General Information | Top | |||||
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Target ID |
T62820
(Former ID: TTDR00321)
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Target Name |
Metabotropic glutamate receptor 2 (mGluR2)
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Synonyms |
mGLUR2; Group II metabotropic glutamate receptor; Glutamate receptor mGLU2; GPRC1B
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Gene Name |
GRM2
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Target Type |
Clinical trial target
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[1] | ||||
Disease | [+] 8 Target-related Diseases | + | ||||
1 | Alzheimer disease [ICD-11: 8A20] | |||||
2 | Obesity [ICD-11: 5B80-5B81] | |||||
3 | Psychotic disorder [ICD-11: 6A20-6A25] | |||||
4 | Bipolar disorder [ICD-11: 6A60] | |||||
5 | Depression [ICD-11: 6A70-6A7Z] | |||||
6 | Epilepsy/seizure [ICD-11: 8A61-8A6Z] | |||||
7 | Mental/behavioural/neurodevelopmental disorder [ICD-11: 6E20-6E8Z] | |||||
8 | Schizophrenia [ICD-11: 6A20] | |||||
Function |
Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling inhibits adenylate cyclase activity. May mediate suppression of neurotransmission or may be involved in synaptogenesis or synaptic stabilization. G-protein coupled receptor for glutamate.
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BioChemical Class |
GPCR glutamate
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UniProt ID | ||||||
Sequence |
MGSLLALLALLLLWGAVAEGPAKKVLTLEGDLVLGGLFPVHQKGGPAEDCGPVNEHRGIQ
RLEAMLFALDRINRDPHLLPGVRLGAHILDSCSKDTHALEQALDFVRASLSRGADGSRHI CPDGSYATHGDAPTAITGVIGGSYSDVSIQVANLLRLFQIPQISYASTSAKLSDKSRYDY FARTVPPDFFQAKAMAEILRFFNWTYVSTVASEGDYGETGIEAFELEARARNICVATSEK VGRAMSRAAFEGVVRALLQKPSARVAVLFTRSEDARELLAASQRLNASFTWVASDGWGAL ESVVAGSEGAAEGAITIELASYPISDFASYFQSLDPWNNSRNPWFREFWEQRFRCSFRQR DCAAHSLRAVPFEQESKIMFVVNAVYAMAHALHNMHRALCPNTTRLCDAMRPVNGRRLYK DFVLNVKFDAPFRPADTHNEVRFDRFGDGIGRYNIFTYLRAGSGRYRYQKVGYWAEGLTL DTSLIPWASPSAGPLPASRCSEPCLQNEVKSVQPGEVCCWLCIPCQPYEYRLDEFTCADC GLGYWPNASLTGCFELPQEYIRWGDAWAVGPVTIACLGALATLFVLGVFVRHNATPVVKA SGRELCYILLGGVFLCYCMTFIFIAKPSTAVCTLRRLGLGTAFSVCYSALLTKTNRIARI FGGAREGAQRPRFISPASQVAICLALISGQLLIVVAWLVVEAPGTGKETAPERREVVTLR CNHRDASMLGSLAYNVLLIALCTLYAFKTRKCPENFNEAKFIGFTMYTTCIIWLAFLPIF YVTSSDYRVQTTTMCVSVSLSGSVVLGCLFAPKLHIILFQPQKNVVSHRAPTSRFGSAAA RASSSLGQGSGSQFVPTVCNGREVVDSTTSSL Click to Show/Hide
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3D Structure | Click to Show 3D Structure of This Target | AlphaFold |
Drugs and Modes of Action | Top | |||||
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Clinical Trial Drug(s) | [+] 9 Clinical Trial Drugs | + | ||||
1 | MP-101 | Drug Info | Phase 2 | Alzheimer disease | [2] | |
2 | Oleoyl-estrone | Drug Info | Phase 2 | Obesity | [3] | |
3 | RO-4995819 | Drug Info | Phase 2 | Major depressive disorder | [4] | |
4 | ADX71149 | Drug Info | Phase 1 | Epilepsy | [5] | |
5 | BCI-632 | Drug Info | Phase 1 | Major depressive disorder | [6] | |
6 | BCI-838 | Drug Info | Phase 1 | Major depressive disorder | [7] | |
7 | JNJ-42491293 | Drug Info | Phase 1 | Psychiatric disorder | [8] | |
8 | LY-2979165 | Drug Info | Phase 1 | Bipolar disorder | [9] | |
9 | Pomaglumetad | Drug Info | Phase 1 | Schizophrenia | [10] | |
Discontinued Drug(s) | [+] 6 Discontinued Drugs | + | ||||
1 | LY-544344 | Drug Info | Discontinued in Phase 3 | Anxiety disorder | [11] | |
2 | LY-2300559 | Drug Info | Discontinued in Phase 2 | Migraine | [12] | |
3 | LY354740 | Drug Info | Discontinued in Phase 2 | Anxiety disorder | [13], [14] | |
4 | R-1578 | Drug Info | Discontinued in Phase 2 | Mood disorder | [15] | |
5 | RG1578 | Drug Info | Discontinued in Phase 2 | Major depressive disorder | [15] | |
6 | TS-032 | Drug Info | Discontinued in Phase 1 | Schizophrenia | [16] | |
Mode of Action | [+] 6 Modes of Action | + | ||||
Agonist | [+] 11 Agonist drugs | + | ||||
1 | MP-101 | Drug Info | [2] | |||
2 | Oleoyl-estrone | Drug Info | [5], [17] | |||
3 | LY-544344 | Drug Info | [25] | |||
4 | LY354740 | Drug Info | [27] | |||
5 | TS-032 | Drug Info | [30] | |||
6 | (1S,3R)-ACPD | Drug Info | [32] | |||
7 | (2R,4R)-4-aminopyrrolidine-2,4-dicarboxylate | Drug Info | [33], [34] | |||
8 | (S)-4C3HPG | Drug Info | [31] | |||
9 | DCG IV | Drug Info | [34] | |||
10 | L-CCG-I | Drug Info | [32] | |||
11 | MGS0028 | Drug Info | [42] | |||
Modulator | [+] 8 Modulator drugs | + | ||||
1 | RO-4995819 | Drug Info | [18] | |||
2 | ADX71149 | Drug Info | [19] | |||
3 | BCI-838 | Drug Info | [21] | |||
4 | LY-2979165 | Drug Info | [23] | |||
5 | Pomaglumetad | Drug Info | [1] | |||
6 | LY-2300559 | Drug Info | [26] | |||
7 | RG1578 | Drug Info | [29] | |||
8 | DT-2228 | Drug Info | [38] | |||
Antagonist | [+] 56 Antagonist drugs | + | ||||
1 | BCI-632 | Drug Info | [20] | |||
2 | Ethinyl-pyrazole derivative 1 | Drug Info | [24] | |||
3 | Ethinyl-pyrazole derivative 2 | Drug Info | [24] | |||
4 | Ethinyl-pyrazole derivative 3 | Drug Info | [24] | |||
5 | Heteroaryl-pyrazole derivative 1 | Drug Info | [24] | |||
6 | Heteroaryl-pyrazole derivative 2 | Drug Info | [24] | |||
7 | Heteroaryl-pyrazole derivative 3 | Drug Info | [24] | |||
8 | N-substituted pyrazole derivative 1 | Drug Info | [24] | |||
9 | N-substituted pyrazole derivative 2 | Drug Info | [24] | |||
10 | N-substituted pyrazole derivative 3 | Drug Info | [24] | |||
11 | PMID25435285-Compound-10 | Drug Info | [24] | |||
12 | PMID25435285-Compound-15 | Drug Info | [24] | |||
13 | PMID25435285-Compound-16 | Drug Info | [24] | |||
14 | PMID25435285-Compound-20 | Drug Info | [24] | |||
15 | PMID25435285-Compound-22 | Drug Info | [24] | |||
16 | PMID25435285-Compound-25 | Drug Info | [24] | |||
17 | PMID25435285-Compound-26 | Drug Info | [24] | |||
18 | PMID25435285-Compound-37 | Drug Info | [24] | |||
19 | PMID25435285-Compound-38 | Drug Info | [24] | |||
20 | PMID25435285-Compound-39 | Drug Info | [24] | |||
21 | PMID25435285-Compound-40 | Drug Info | [24] | |||
22 | PMID25435285-Compound-41 | Drug Info | [24] | |||
23 | PMID25435285-Compound-42 | Drug Info | [24] | |||
24 | PMID25435285-Compound-43 | Drug Info | [24] | |||
25 | PMID25435285-Compound-44 | Drug Info | [24] | |||
26 | PMID25435285-Compound-45 | Drug Info | [24] | |||
27 | PMID25435285-Compound-46 | Drug Info | [24] | |||
28 | PMID25435285-Compound-47 | Drug Info | [24] | |||
29 | PMID25435285-Compound-49 | Drug Info | [24] | |||
30 | PMID25435285-Compound-50 | Drug Info | [24] | |||
31 | PMID25435285-Compound-51 | Drug Info | [24] | |||
32 | PMID25435285-Compound-52 | Drug Info | [24] | |||
33 | PMID25435285-Compound-53 | Drug Info | [24] | |||
34 | Pyrazole derivative 76 | Drug Info | [24] | |||
35 | Pyrazole derivative 77 | Drug Info | [24] | |||
36 | Pyrazole derivative 78 | Drug Info | [24] | |||
37 | Pyrazole derivative 79 | Drug Info | [24] | |||
38 | Quinoline derivative 3 | Drug Info | [24] | |||
39 | Quinoline derivative 4 | Drug Info | [24] | |||
40 | Quinoline derivative 5 | Drug Info | [24] | |||
41 | Quinoline derivative 6 | Drug Info | [24] | |||
42 | Quinoline derivative 7 | Drug Info | [24] | |||
43 | Quinoline derivative 8 | Drug Info | [24] | |||
44 | Quinoline derivative 9 | Drug Info | [24] | |||
45 | Tetra-hydro-imidazo[1,5-d][1,4]oxazepin-3-yl derivative 1 | Drug Info | [24] | |||
46 | Tetra-hydro-imidazo[1,5-d][1,4]oxazepin-3-yl derivative 2 | Drug Info | [24] | |||
47 | Tetra-hydro-imidazo[1,5-d][1,4]oxazepin-3-yl derivative 3 | Drug Info | [24] | |||
48 | Tetra-hydro-imidazo[1,5-d][1,4]oxazepin-3-yl derivative 4 | Drug Info | [24] | |||
49 | Tetra-hydro-imidazo[1,5-d][1,4]oxazepin-3-yl derivative 5 | Drug Info | [24] | |||
50 | Tetra-hydro-imidazo[1,5-d][1,4]oxazepin-3-yl derivative 6 | Drug Info | [24] | |||
51 | R-1578 | Drug Info | [28] | |||
52 | (+)-MCPG | Drug Info | [31] | |||
53 | alpha-methylserine-O-phosphate | Drug Info | [31] | |||
54 | eGlu | Drug Info | [27] | |||
55 | PCCG-4 | Drug Info | [44] | |||
56 | [3H]LY341495 | Drug Info | [32], [33] | |||
Binder | [+] 1 Binder drugs | + | ||||
1 | JNJ-42491293 | Drug Info | [22] | |||
Modulator (allosteric modulator) | [+] 22 Modulator (allosteric modulator) drugs | + | ||||
1 | 3-MPPTS | Drug Info | [35] | |||
2 | 4-APPES | Drug Info | [35] | |||
3 | 4-MPPTS | Drug Info | [36] | |||
4 | biphenylindanone A | Drug Info | [37] | |||
5 | CBiPES | Drug Info | [35] | |||
6 | cyPPTS | Drug Info | [35] | |||
7 | GSK1331268 | Drug Info | [39] | |||
8 | JNJ-42153605 | Drug Info | [40] | |||
9 | MNI-135 | Drug Info | [43] | |||
10 | MNI-136 | Drug Info | [43] | |||
11 | MNI-137 | Drug Info | [43] | |||
12 | PMID20409708C34 | Drug Info | [45] | |||
13 | PMID21155570C14 | Drug Info | [46] | |||
14 | PMID22364337C48 | Drug Info | [47] | |||
15 | PTBE | Drug Info | [48] | |||
16 | Ro4491533 | Drug Info | [49] | |||
17 | RO4988546 | Drug Info | [50] | |||
18 | RO5488608 | Drug Info | [50] | |||
19 | Ro64-5229 | Drug Info | [51] | |||
20 | THIIC | Drug Info | [52] | |||
21 | [3H]2,2,2-TEMPS | Drug Info | [36], [50] | |||
22 | [3H]JNJ-40068782 | Drug Info | [53] | |||
Inhibitor | [+] 3 Inhibitor drugs | + | ||||
1 | LY-379268 | Drug Info | [41] | |||
2 | LY-389795 | Drug Info | [41] | |||
3 | [3H]quisqualate | Drug Info | [54] |
Chemical Structure based Activity Landscape of Target | Top |
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Drug Property Profile of Target | Top | |
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(1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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(5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five |
Co-Targets | Top | |||||
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Co-Targets |
Target Poor or Non Binders | Top | |||||
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Target Poor or Non Binders |
Target Profiles in Patients | Top | |||||
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Target Expression Profile (TEP) |
Target Affiliated Biological Pathways | Top | |||||
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KEGG Pathway | [+] 3 KEGG Pathways | + | ||||
1 | Neuroactive ligand-receptor interaction | |||||
2 | Glutamatergic synapse | |||||
3 | Cocaine addiction | |||||
Panther Pathway | [+] 4 Panther Pathways | + | ||||
1 | Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway | |||||
2 | Heterotrimeric G-protein signaling pathway-Gq alpha and Go alpha mediated pathway | |||||
3 | Ionotropic glutamate receptor pathway | |||||
4 | Metabotropic glutamate receptor group II pathway | |||||
Reactome | [+] 2 Reactome Pathways | + | ||||
1 | G alpha (i) signalling events | |||||
2 | Class C/3 (Metabotropic glutamate/pheromone receptors) | |||||
WikiPathways | [+] 3 WikiPathways | + | ||||
1 | GPCRs, Class C Metabotropic glutamate, pheromone | |||||
2 | GPCR ligand binding | |||||
3 | GPCR downstream signaling |
Target-Related Models and Studies | Top | |||||
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Target Validation |
References | Top | |||||
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REF 1 | LY-2140023, a prodrug of the group II metabotropic glutamate receptor agonist LY-404039 for the potential treatment of schizophrenia. Curr Opin Investig Drugs. 2010 Jul;11(7):833-45. | |||||
REF 2 | ClinicalTrials.gov (NCT03044249) A Study of MP-101 in Dementia-Related Psychosis and/or Agitation and Aggression. U.S. National Institutes of Health. | |||||
REF 3 | ClinicalTrials.gov (NCT00449202) Phase 2a Obesity Study of Oral Doses of Oleoyl-Estrone (MP-101). U.S. National Institutes of Health. | |||||
REF 4 | ClinicalTrials.gov (NCT01457677) ARTDeCo Study: A Study of RO4995819 in Patients With Major Depressive Disorder And Inadequate Response to Ongoing Antidepressant Treatment in Hoffmann-La Roche. | |||||
REF 5 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 6 | ClinicalTrials.gov (NCT01548703) A Multiple Ascending Dose Study of BCI-838 in Healthy Volunteers. U.S. National Institutes of Health. | |||||
REF 7 | ClinicalTrials.gov (NCT01548703) A Multiple Ascending Dose Study of BCI-838 in Healthy Volunteers in BrainCells Inc. | |||||
REF 8 | ClinicalTrials.gov (NCT01359852) A Study of [11C]JNJ-42491293, a Possible PET Ligand for the mGlu2 Receptor, in Healthy Adult Volunteers in Healthy Volunteers in Johnson & Johnson Pharmaceutical Research & Development, L.L.C. | |||||
REF 9 | ClinicalTrials.gov (NCT01248052) A First Human Dose Study to Investigate Safety and Tolerability of LY2979165 in Healthy Volunteers in Eli Lilly and Company. | |||||
REF 10 | ClinicalTrials.gov (NCT01487083) A Long-Term Study in Schizophrenia. U.S. National Institutes of Health. | |||||
REF 11 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018821) | |||||
REF 12 | ClinicalTrials.gov (NCT01184508) A Study in Migraine Prevention. U.S. National Institutes of Health. | |||||
REF 13 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1393). | |||||
REF 14 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008428) | |||||
REF 15 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800034342) | |||||
REF 16 | ClinicalTrials.gov (NCT00876304) Multiple Dose Safety Study of PF-04802540 in Subjects With Schizophrenia. U.S. National Institutes of Health. | |||||
REF 17 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 18 | Novel glutamatergic drugs for the treatment of mood disorders. Neuropsychiatr Dis Treat. 2013; 9: 1101-1112. | |||||
REF 19 | MGlu2 receptor-mediated modulation of conditioned avoidance behavior in rats. European journal of pharmacology. 01/2014; 727(1). | |||||
REF 20 | Synthesis, in vitro pharmacology, structure-activity relationships, and pharmacokinetics of 3-alkoxy-2-amino-6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent and selective group II metabotropic glutamate receptor antagonists. J Med Chem. 2004 Aug 26;47(18):4570-87. | |||||
REF 21 | Metabotropic glutamate receptor subtype 2 (GRM2; MGLUR2); GRM3 (MGLUR3). SciBX 3(13); doi:10.1038/scibx.2010.413. April 1 2010 | |||||
REF 22 | Opportunities and challenges in the discovery of allosteric modulators of GPCRs for treating CNS disorders. Nat Rev Drug Discov. 2014 Sep;13(9):692-708. | |||||
REF 23 | Annual Reports in Medicinal Chemistry. Volume 47, 2012, Page(78). | |||||
REF 24 | Novel metabotropic glutamate receptor 2/3 antagonists and their therapeutic applications: a patent review (2005 - present).Expert Opin Ther Pat. 2015 Jan;25(1):69-90. | |||||
REF 25 | Glutamate- and GABA-based CNS therapeutics. Curr Opin Pharmacol. 2006 Feb;6(1):7-17. | |||||
REF 26 | Annual Reports in Medicinal Chemistry. Elsevier (ISBN: 9780123964922). 2012, p78 | |||||
REF 27 | Characterization of [(3)H]-LY354740 binding to rat mGlu2 and mGlu3 receptors expressed in CHO cells using semliki forest virus vectors. Neuropharmacology. 2000 Jul 24;39(10):1700-6. | |||||
REF 28 | Clinical pipeline report, company report or official report of Roche. | |||||
REF 29 | Company report (Roche pipeline: 15 April 2014) | |||||
REF 30 | Metabotropic glutamate receptor subtype 2/3 (mGluR2/3); serotonin receptor (5-HT2A receptor). SciBX 1(6); doi:10.1038/scibx.2008.145. March 6 2008 | |||||
REF 31 | Characterization of [3H]-(2S,2'R,3'R)-2-(2',3'-dicarboxy-cyclopropyl)glycine ([3H]-DCG IV) binding to metabotropic mGlu2 receptor-transfected cell membranes. Br J Pharmacol. 1998 Feb;123(3):497-504. | |||||
REF 32 | [3H]-LY341495 as a novel antagonist radioligand for group II metabotropic glutamate (mGlu) receptors: characterization of binding to membranes of mGlu receptor subtype expressing cells. Neuropharmacology. 1999 Oct;38(10):1519-29. | |||||
REF 33 | Group II metabotropic glutamate receptors within the amygdala regulate fear as assessed with potentiated startle in rats. Behav Neurosci. 2002 Dec;116(6):1075-83. | |||||
REF 34 | Attenuation of seizures induced by homocysteic acid in immature rats by metabotropic glutamate group II and group III receptor agonists. Brain Res. 2001 Jul 27;908(2):120-9. | |||||
REF 35 | Metabotropic glutamate 2 receptor potentiators: receptor modulation, frequency-dependent synaptic activity, and efficacy in preclinical anxiety and... Psychopharmacology (Berl). 2005 Apr;179(1):271-83. | |||||
REF 36 | SAR study of a subtype selective allosteric potentiator of metabotropic glutamate 2 receptor, N-(4-phenoxyphenyl)-N-(3-pyridinylmethyl)ethanesulfonamide. Bioorg Med Chem Lett. 2004 Jun 21;14(12):3099-102. | |||||
REF 37 | Biphenyl-indanones: allosteric potentiators of the metabotropic glutamate subtype 2 receptor. Bioorg Med Chem Lett. 2005 Oct 1;15(19):4354-8. | |||||
REF 38 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 290). | |||||
REF 39 | The identification of structurally novel, selective, orally bioavailable positive modulators of mGluR2. Bioorg Med Chem Lett. 2010 Jan 15;20(2):759-62. | |||||
REF 40 | Discovery of 3-cyclopropylmethyl-7-(4-phenylpiperidin-1-yl)-8-trifluoromethyl[1,2,4]triazolo[4,3-a]pyridine (JNJ-42153605): a positive allosteric modulator of the metabotropic glutamate 2 receptor. JMed Chem. 2012 Oct 25;55(20):8770-89. | |||||
REF 41 | Synthesis and metabotropic glutamate receptor activity of S-oxidized variants of (-)-4-amino-2-thiabicyclo-[3.1.0]hexane-4,6-dicarboxylate: identif... J Med Chem. 2007 Jan 25;50(2):233-40. | |||||
REF 42 | Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists. J Med Chem. 2000 Dec 14;43(25):4893-909. | |||||
REF 43 | A novel family of potent negative allosteric modulators of group II metabotropic glutamate receptors. J Pharmacol Exp Ther. 2007 Jul;322(1):254-64. | |||||
REF 44 | 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 receptors antagonist. J Med Chem. 1996 May 24;39(11):2259-69. | |||||
REF 45 | 3-Aryl-5-phenoxymethyl-1,3-oxazolidin-2-ones as positive allosteric modulators of mGluR2 for the treatment of schizophrenia: Hit-to-lead efforts. Bioorg Med Chem Lett. 2010 May 15;20(10):3129-33. | |||||
REF 46 | Design and synthesis of an orally active metabotropic glutamate receptor subtype-2 (mGluR2) positive allosteric modulator (PAM) that decreases cocaine self-administration in rats. J Med Chem. 2011 Jan 13;54(1):342-53. | |||||
REF 47 | Discovery of 1,4-disubstituted 3-cyano-2-pyridones: a new class of positive allosteric modulators of the metabotropic glutamate 2 receptor. J Med Chem. 2012 Mar 8;55(5):2388-405. | |||||
REF 48 | Phenyl-tetrazolyl acetophenones: discovery of positive allosteric potentiatiors for the metabotropic glutamate 2 receptor. J Med Chem. 2004 Aug 26;47(18):4595-9. | |||||
REF 49 | Characterization of an mGluR2/3 negative allosteric modulator in rodent models of depression. J Neurogenet. 2011 Dec;25(4):152-66. | |||||
REF 50 | Structural determinants of allosteric antagonism at metabotropic glutamate receptor 2: mechanistic studies with new potent negative allosteric modulators. Br J Pharmacol. 2011 Sep;164(2b):521-37. | |||||
REF 51 | Synthesis of heterocyclic enol ethers and their use as group 2 metabotropic glutamate receptor antagonists. Bioorg Med Chem Lett. 1999 Aug 2;9(15):2173-6. | |||||
REF 52 | N-(4-((2-(trifluoromethyl)-3-hydroxy-4-(isobutyryl)phenoxy)methyl)benzyl)-1-methyl-1H-imidazole-4-carboxamide (THIIC), a novel metabotropic glutamate 2 potentiator with potential anxiolytic/antidepressant properties: in vivo profiling suggests a link between behavioral and central nervous system neurochemical changes. J Pharmacol Exp Ther. 2011 Jan;336(1):165-77. | |||||
REF 53 | Pharmacological characterization of JNJ-40068782, a new potent, selective, and systemically active positive allosteric modulator of the mGlu2 receptor and its radioligand [3H]JNJ-40068782. J Pharmacol Exp Ther. 2013 Sep;346(3):514-27. | |||||
REF 54 | Excitatory amino acid receptor ligands: resolution, absolute stereochemistry, and enantiopharmacology of 2-amino-3-(4-butyl-3-hydroxyisoxazol-5-yl)... J Med Chem. 1998 Mar 12;41(6):930-9. |
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