The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 28212015 |
51 |
Discovery and Preclinical Characterization of 3-((4-(4-Chlorophenyl)-7-fluoroquinoline-3-yl)sulfonyl)benzonitrile, a Novel Non-acetylenic Metabotropic Glutamate Receptor 5 (mGluR5) Negative Allosteric Modulator for Psychiatric Indications. |
Gedeon Richter |
| 28109949 |
10 |
Positional isomers of bispyridine benzene derivatives induce efficacy changes on mGlu |
Institute For Advanced Chemistry of Catalonia (Iqac-Csic) |
| 27994742 |
34 |
Development of 1 |
Bristol-Myers Squibb |
| 26985317 |
20 |
Discovery and Preclinical Evaluation of BMS-955829, a Potent Positive Allosteric Modulator of mGluR5. |
Bristol-Myers Squibb Research & Development |
| 26988308 |
130 |
N-Alkylpyrido[1',2':1,5]pyrazolo-[4,3-d]pyrimidin-4-amines: A new series of negative allosteric modulators of mGlu1/5 with CNS exposure in rodents. |
Vanderbilt University Medical Center |
| 26814576 |
146 |
New 4-Functionalized Glutamate Analogues Are Selective Agonists at Metabotropic Glutamate Receptor Subtype 2 or Selective Agonists at Metabotropic Glutamate Receptor Group III. |
University of Copenhagen |
| 26706173 |
13 |
7TM X-ray structures for class C GPCRs as new drug-discovery tools. 1. mGluR5. |
Shenyang Pharmaceutical University |
| 26774652 |
12 |
4-Aryl-3-arylsulfonyl-quinolines as negative allosteric modulators of metabotropic GluR5 receptors: From HTS hit to development candidate. |
Gedeon Richter |
| 26516782 |
59 |
Selective Allosteric Antagonists for the G Protein-Coupled Receptor GPRC6A Based on the 2-Phenylindole Privileged Structure Scaffold. |
University of Copenhagen |
| 26475522 |
81 |
Acyl dihydropyrazolo[1,5-a]pyrimidinones as metabotropic glutamate receptor 5 positive allosteric modulators. |
Vanderbilt University Medical Center |
| 26335039 |
320 |
Discovery of a Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents. |
Vanderbilt University Medical Center |
| 26014480 |
87 |
Insights into the interaction of negative allosteric modulators with the metabotropic glutamate receptor 5: discovery and computational modeling of a new series of ligands with nanomolar affinity. |
University of Modena and Reggio Emilia |
| 25958247 |
22 |
Synthesis and studies on the mGluR agonist activity of FAP4 stereoisomers. |
Univ. Rouen |
| 25791451 |
126 |
Thieno[2,3-b]pyridines as negative allosteric modulators of metabotropic GluR5 receptors: Lead optimization. |
Gedeon Richter |
| 25683622 |
86 |
Discovery and SAR of novel series of imidazopyrimidinones and dihydroimidazopyrimidinones as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5). |
Janssen Pharmaceutica |
| 25017030 |
17 |
Thieno[2,3-b]pyridines as negative allosteric modulators of metabotropic GluR5 receptors: hit-to-lead optimization. |
Gedeon Richter |
| 24969015 |
118 |
Discovery of VU0431316: a negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety. |
Vanderbilt University Medical Center |
| 24961642 |
82 |
Discovery and SAR of a novel series of metabotropic glutamate receptor 5 positive allosteric modulators with high ligand efficiency. |
Vanderbilt University Medical Center |
| 24914612 |
36 |
Tetrahydronaphthyridine and dihydronaphthyridinone ethers as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5). |
Vanderbilt University Medical Center |
| 23374867 |
40 |
Discovery of (1R,2R)-N-(4-(6-isopropylpyridin-2-yl)-3-(2-methyl-2H-indazol-5-yl)isothiazol-5-yl)-2-methylcyclopropanecarboxamide, a potent and orally efficacious mGlu5 receptor negative allosteric modulator. |
Eli Lilly |
| 22924094 |
41 |
Metabotropic glutamate receptor 5 negative allosteric modulators as novel tools for in vivo investigation. |
TBA |
| 20732812 |
118 |
3D-QSAR CoMFA study of benzoxazepine derivatives as mGluR5 positive allosteric modulators. |
Vanderbilt University |
| 20483612 |
41 |
Hit-to-lead optimization of disubstituted oxadiazoles and tetrazoles as mGluR5 NAMs. |
Gedeon Richter |
| 23142615 |
35 |
Discovery and SAR of a novel series of non-MPEP site mGlu5 PAMs based on an aryl glycine sulfonamide scaffold. |
Vanderbilt University Medical Center |
| 22607673 |
34 |
Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM. |
Vanderbilt University Medical Center |
| 23194448 |
9 |
Development of N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methyl-4-[11C]methylbenzamide for positron emission tomography imaging of metabotropic glutamate 1 receptor in monkey brain. |
National Institute of Radiological Sciences |
| 23009245 |
53 |
Orally active metabotropic glutamate subtype 2 receptor positive allosteric modulators: structure-activity relationships and assessment in a rat model of nicotine dependence. |
Sanford-Burnham Medical Research Institute |
| 23046966 |
43 |
Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
Astrazeneca |
| 22822714 |
6 |
Synthesis and evaluation of novela-fluorinated (E)-3-((6-methylpyridin-2-yl)ethynyl)cyclohex-2-enone-O-methyl oxime (ABP688) derivatives as metabotropic glutamate receptor subtype 5 PET radiotracers. |
Institute of Technology (Eth) Zurich |
| 22981332 |
58 |
Optimization of an ether series of mGlu5 positive allosteric modulators: molecular determinants of MPEP-site interaction crossover. |
Vanderbilt University Medical Center |
| 22316010 |
12 |
Synthesis and evaluation of novel radioligands for positron emission tomography imaging of metabotropic glutamate receptor subtype 1 (mGluR1) in rodent brain. |
National Institute of Radiological Sciences |
| 21207959 |
69 |
Syntheses of 2-amino and 2-halothiazole derivatives as high-affinity metabotropic glutamate receptor subtype 5 ligands and potential radioligands for in vivo imaging. |
National Institute of Mental Health |
| 18793851 |
4 |
Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4): Part I. Discovery of pyrazolo[3,4-d]pyrimidines as novel mGluR4 positive allosteric modulators. |
Vanderbilt University Medical Center |
| 18578478 |
60 |
Chemo-enzymatic synthesis of a series of 2,4-syn-functionalized (S)-glutamate analogues: new insight into the structure-activity relation of ionotropic glutamate receptor subtypes 5, 6, and 7. |
Universite Blaise Pascal |
| 18173231 |
71 |
Positive and negative modulation of group I metabotropic glutamate receptors. |
Institute of Organic Synthesis |
| 17210250 |
45 |
Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA. |
Merck |
| 17350267 |
48 |
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. |
Universit£ |
| 17110115 |
13 |
ABP688, a novel selective and high affinity ligand for the labeling of mGlu5 receptors: identification, in vitro pharmacology, pharmacokinetic and biodistribution studies. |
Novartis Institutes For Biomedical Research |
| 16213710 |
32 |
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. |
Universit£ |
| 9357538 |
38 |
(S)-homo-AMPA, a specific agonist at the mGlu6 subtype of metabotropic glutamic acid receptors. |
Royal Danish School of Pharmacy |
| 7738999 |
88 |
Metabotropic glutamate receptors: novel targets for drug development. |
Cns Research |
| 12565928 |
11 |
[3H]-methoxymethyl-MTEP and [3H]-methoxy-PEPy: potent and selective radioligands for the metabotropic glutamate subtype 5 (mGlu5) receptor. |
Merck Research Laboratories |
| 21966889 |
61 |
Discovery, synthesis, and structure-activity relationship development of a series of N-4-(2,5-dioxopyrrolidin-1-yl)phenylpicolinamides (VU0400195, ML182): characterization of a novel positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu(4)) with oral efficacy in an antiparkin |
Vanderbilt University Medical Center |
| 21546249 |
42 |
Potent mGluR5 antagonists: pyridyl and thiazolyl-ethynyl-3,5-disubstituted-phenyl series. |
Institute For Neurodegenerative Disorders |
| 21295978 |
22 |
Design and synthesis of substituted N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides as positive allosteric modulators of the metabotropic glutamate receptor subtype 5. |
National Institute On Drug Abuse-Intramural Research Program |
| 21183344 |
59 |
Discovery of molecular switches within the ADX-47273 mGlu5 PAM scaffold that modulate modes of pharmacology to afford potent mGlu5 NAMs, PAMs and partial antagonists. |
Vanderbilt University Medical Center |
| 23308336 |
13 |
Discovery of N-Aryl Piperazines as Selective mGlu(5) Potentiators with Efficacy in a Rodent Model Predictive of Anti-Psychotic Activity. |
TBA |
| 24900255 |
19 |
Benzimidazoles as Potent and Orally Active mGlu5 Receptor Antagonists with an Improved PK Profile |
TBA |
| 21126874 |
38 |
3-(Pyridin-2-yl-ethynyl)benzamide metabotropic glutamate receptor 5 negative allosteric modulators: hit to lead studies. |
Pfizer |
| 20809633 |
16 |
Design, synthesis, and structure-activity relationships of novel bicyclic azole-amines as negative allosteric modulators of metabotropic glutamate receptor 5. |
Sepracor |
| 20634080 |
4 |
Syntheses and pharmacological characterization of novel thiazole derivatives as potential mGluR5 PET ligands. |
Eth Zurich (Swiss Federal Institute of Technology) |
| 20638279 |
46 |
An orally bioavailable positive allosteric modulator of the mGlu4 receptor with efficacy in an animal model of motor dysfunction. |
Evotec (Uk) |
| 20615697 |
49 |
Carbamoyloximes as novel non-competitive mGlu5 receptor antagonists. |
Gedeon Richter |
| 20598884 |
48 |
3-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu(5): Identification of easily prepared tool compounds with CNS exposure in rats. |
Vanderbilt University Medical Center |
| 20411954 |
17 |
Structure-activity relationships of fluorinated (E)-3-((6-methylpyridin-2-yl)ethynyl)cyclohex-2-enone-O-methyloxime (ABP688) derivatives and the discovery of a high affinity analogue as a potential candidate for imaging metabotropic glutamate recepors subtype 5 (mGluR5) with positron emission tomog |
Eth Zurich |
| 20382541 |
31 |
Structure-activity relationships in a novel series of 7-substituted-aryl quinolines and 5-substituted-aryl benzothiazoles at the metabotropic glutamate receptor subtype 5. |
National Institute On Drug Abuse-Intramural Research Program |
| 20346665 |
30 |
A-ring modifications on the triazafluorenone core structure and their mGluR1 antagonist properties. |
Merck Research Laboratories |
| 19875287 |
56 |
Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS. |
Vanderbilt University Medical Center |
| 19854049 |
49 |
Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5. |
Vanderbilt University Medical Center |
| 19931453 |
59 |
Piperidyl amides as novel, potent and orally active mGlu5 receptor antagonists with anxiolytic-like activity. |
Novartis Institutes For Biomedical Research |
| 19574055 |
82 |
Synergism of virtual screening and medicinal chemistry: identification and optimization of allosteric antagonists of metabotropic glutamate receptor 1. |
Merz Pharmaceuticals |
| | 6 |
Synthesis and biological activity of cyclic analogues of MPPG and MCPG as metabotropic glutamate receptor antagonists |
TBA |
| | 15 |
Synthesis, molecular modeling, and biology of the 1-benzyl derivative of APDC-an apparent mGluR6 selective ligand |
TBA |
| 19537763 |
24 |
Discovery of molecular switches that modulate modes of metabotropic glutamate receptor subtype 5 (mGlu5) pharmacology in vitro and in vivo within a series of functionalized, regioisomeric 2- and 5-(phenylethynyl)pyrimidines. |
Vanderbilt University Medical Center |
| 19445453 |
87 |
Structure-activity relationships comparing N-(6-methylpyridin-yl)-substituted aryl amides to 2-methyl-6-(substituted-arylethynyl)pyridines or 2-methyl-4-(substituted-arylethynyl)thiazoles as novel metabotropic glutamate receptor subtype 5 antagonists. |
National Institute On Drug Abuse-Intramural Research Program |
| 18550372 |
14 |
Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold. |
Vanderbilt University Medical Center |
| 17936624 |
30 |
Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists. |
Pfizer |
| 17723296 |
23 |
Synthesis and SAR of 2-aryl pyrido[2,3-d]pyrimidines as potent mGlu5 receptor antagonists. |
Pfizer |
| 17590335 |
39 |
Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists. |
Pfizer |
| 17571866 |
49 |
Synthesis and simple 18F-labeling of 3-fluoro-5-(2-(2-(fluoromethyl)thiazol-4-yl)ethynyl)benzonitrile as a high affinity radioligand for imaging monkey brain metabotropic glutamate subtype-5 receptors with positron emission tomography. |
National Institute of Mental Health |
| 17446071 |
15 |
Discovery of heterobicyclic templates for novel metabotropic glutamate receptor subtype 5 antagonists. |
National Institute On Drug Abuse |
| 17336520 |
16 |
Design and synthesis of novel heterobiaryl amides as metabotropic glutamate receptor subtype 5 antagonists. |
National Institute On Drug Abuse |
| 16828551 |
12 |
Design and synthesis of APTCs (aminopyrrolidinetricarboxylic acids): identification of a new group III metabotropic glutamate receptor selective agonist. |
Faust Pharmaceuticals |
| 16809035 |
15 |
Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists. |
Abbott Laboratories |
| 16722652 |
95 |
Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes. |
Vanderbilt University School of Medicine |
| 16678408 |
32 |
Design and synthesis of noncompetitive metabotropic glutamate receptor subtype 5 antagonists. |
National Institute On Drug Abuse |
| 16451073 |
63 |
Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications. |
University of Illinois At Chicago |
| 16380255 |
42 |
Phenyl ureas of creatinine as mGluR5 antagonists. A structure-activity relationship study of fenobam analogues. |
Astrazeneca R&D |
| 16279797 |
132 |
Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists. |
Abbott Laboratories |
| 16183275 |
42 |
3-[Substituted]-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitriles: identification of highly potent and selective metabotropic glutamate subtype 5 receptor antagonists. |
Merck Research Laboratories |
| 16115767 |
64 |
Cyclohexenyl- and dehydropiperidinyl-alkynyl pyridines as potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists. |
Merck Research Laboratories |
| 16078827 |
2 |
A positron emission tomography radioligand for the in vivo labeling of metabotropic glutamate 1 receptor: (3-ethyl-2-[11C]methyl-6-quinolinyl)(cis- 4-methoxycyclohexyl)methanone. |
Columbia University College of Physicians and Surgeons |
| 15686891 |
45 |
Functionalization at position 3 of the phenyl ring of the potent mGluR5 noncompetitive antagonists MPEP. |
Yale University |
| 15537338 |
38 |
Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo. |
Merck Research Laboratories |
| 15482908 |
13 |
Discovery of highly potent, selective, orally bioavailable, metabotropic glutamate subtype 5 (mGlu5) receptor antagonists devoid of cytochrome P450 1A2 inhibitory activity. |
Merck Research Laboratories |
| 15482907 |
36 |
3-[3-Fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)phenyl]-4-methylpyridine: a highly potent and orally bioavailable metabotropic glutamate subtype 5 (mGlu5) receptor antagonist. |
Merck Research Laboratories |
| 15482906 |
25 |
2-(2-[3-(pyridin-3-yloxy)phenyl]-2H-tetrazol-5-yl) pyridine: a highly potent, orally active, metabotropic glutamate subtype 5 (mGlu5) receptor antagonist. |
Merck Research Laboratories |
| 15341479 |
36 |
Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity. |
TBA |
| 15317467 |
105 |
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. |
Taisho Pharmaceutical |
| 15225713 |
36 |
5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist with anxiolytic activity. |
Merck Research Laboratories |
| 14711315 |
72 |
(2S,1'S,2'R,3'R)-2-(2'-Carboxy-3'-hydroxymethylcyclopropyl) glycine is a highly potent group 2 and 3 metabotropic glutamate receptor agonist with oral activity. |
Eli Lilly |
| 12825948 |
13 |
Synthesis and anticonvulsant activity of novel bicyclic acidic amino acids. |
Università |
| 12519057 |
22 |
3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-pyridine: a potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity. |
Merck Research Laboratories |
| 12213064 |
33 |
Selective agonists at group II metabotropic glutamate receptors: synthesis, stereochemistry, and molecular pharmacology of (S)- and (R)-2-amino-4-(4-hydroxy[1,2,5]thiadiazol-3-yl)butyric acid. |
The Royal Danish School of Pharmacy |
| 11831912 |
43 |
Selective antagonists at group I metabotropic glutamate receptors: synthesis and molecular pharmacology of 4-aryl-3-isoxazolol amino acids. |
The Royal Danish School of Pharmacy |
| 31789518 |
11 |
Urea Derivatives in Modern Drug Discovery and Medicinal Chemistry. |
Purdue University |
| 29939744 |
179 |
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential. |
Shanghaitech University |
| 23850200 |
36 |
A novel series of metabotropic glutamate receptor 5 negative allosteric modulators based on a 4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine core. |
Addex Therapeutics |
| 24900698 |
4 |
Negative allosteric modulators of metabotropic glutamate receptor subtype. |
Dart Neuroscience |
| 29705142 |
58 |
Discovery of 6-(pyrimidin-5-ylmethyl)quinoline-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5. |
Vanderbilt University |
| 29057060 |
100 |
Discovery of VU6005649, a CNS Penetrant mGlu |
Vanderbilt University |
| 28947938 |
63 |
Design and Synthesis of |
Vanderbilt University School of Medicine |
| 28390229 |
14 |
Discovery of 4-amino-3-arylsulfoquinolines, a novel non-acetylenic chemotype of metabotropic glutamate 5 (mGlu |
Gedeon Richter |
| 28958625 |
88 |
Discovery of imidazo[1,2-a]-, [1,2,4]triazolo[4,3-a]-, and [1,2,4]triazolo[1,5-a]pyridine-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5. |
Vanderbilt University |
| 28530802 |
121 |
Discovery of N-(5-Fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide (VU0424238): A Novel Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Selected for Clinical Evaluation. |
Vanderbilt University Institute of Imaging Science |
| 28817277 |
34 |
Discovery and Characterization of (R)-6-Neopentyl-2-(pyridin-2-ylmethoxy)-6,7-dihydropyrimido[2,1-c][1,4]oxazin-4(9H)-one (PF-06462894), an Alkyne-Lacking Metabotropic Glutamate Receptor 5 Negative Allosteric Modulator Profiled in both Rat and Nonhuman Primates. |
Pfizer |
| 28244987 |
10 |
Capzimin is a potent and specific inhibitor of proteasome isopeptidase Rpn11. |
California Institute of Technology |
| 26010139 |
34 |
Synthesis and anticholinergic activity of 4-hydroxycoumarin derivatives containing substituted benzyl-1,2,3-triazole moiety. |
Tehran University of Medical Sciences |
| 11071707 |
71 |
Amphetamine-type central nervous system stimulants release norepinephrine more potently than they release dopamine and serotonin. |
Nih |
| 28425720 |
3 |
A Cereblon Modulator (CC-220) with Improved Degradation of Ikaros and Aiolos. |
Celgene |
| 10514285 |
66 |
Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues. |
Medivir |
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