The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
27836401 |
57 |
Novel bicyclo[3.1.0]hexane analogs as antagonists of metabotropic glutamate 2/3 receptors for the treatment of depression. |
Eli Lilly |
27234146 |
66 |
Discovery and characterization of a novel series of N-phenylsulfonyl-1H-pyrrole picolinamides as positive allosteric modulators of the metabotropic glutamate receptor 4 (mGlu4). |
Vanderbilt University Medical Center |
26985321 |
54 |
Optimization of Novel Aza-benzimidazolone mGluR2 PAMs with Respect to LLE and PK Properties and Mitigation of CYP TDI. |
Merck Research Laboratories |
27131990 |
59 |
Discovery of 3-aminopicolinamides as metabotropic glutamate receptor subtype 4 (mGlu4) positive allosteric modulator warheads engendering CNS exposure and in vivo efficacy. |
Vanderbilt University Medical Center |
26988302 |
104 |
Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 3. Engineering plasma stability by discovery and optimization of isoindolinone analogs. |
Vanderbilt University Medical Center |
26810316 |
29 |
Discovery of 5-aryl-1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-ones as positive allosteric modulators of metabotropic glutamate subtype-2 (mGlu2) receptors with efficacy in a preclinical model of psychosis. |
Merck Research Laboratories |
26778256 |
145 |
Lead optimization of the VU0486321 series of mGlu(1) PAMs. Part 2: SAR of alternative 3-methyl heterocycles and progress towards an in vivo tool. |
Vanderbilt University Medical Center |
26684851 |
86 |
Preliminary investigation of 6,7-dihydropyrazolo[1,5-a]pyrazin-4-one derivatives as a novel series of mGlu5 receptor positive allosteric modulators with efficacy in preclinical models of schizophrenia. |
Janssen Pharmaceutica |
26476971 |
117 |
Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 1: SAR of modifications to the central aryl core. |
Vanderbilt University Medical Center |
26475522 |
81 |
Acyl dihydropyrazolo[1,5-a]pyrimidinones as metabotropic glutamate receptor 5 positive allosteric modulators. |
Vanderbilt University Medical Center |
26426481 |
114 |
Development of Novel, CNS Penetrant Positive Allosteric Modulators for the Metabotropic Glutamate Receptor Subtype 1 (mGlu1), Based on an N-(3-Chloro-4-(1,3-dioxoisoindolin-2-yl)phenyl)-3-methylfuran-2-carboxamide Scaffold, That Potentiate Wild Type and Mutant mGlu1 Receptors Found in Schizophrenics |
Vanderbilt University |
26313429 |
155 |
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 (LY2812223), a Highly Potent, Functionally Selective |
Eli Lilly |
26231155 |
53 |
Re-exploring the N-phenylpicolinamide derivatives to develop mGlu4 ligands with improved affinity and in vitro microsomal stability. |
Massachusetts General Hospital |
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 |
25330258 |
18 |
Radiosynthesis and evaluation of an 18F-labeled positron emission tomography (PET) radioligand for metabotropic glutamate receptor subtype 4 (mGlu4). |
Massachusetts General Hospital |
24900783 |
2 |
Qualification of LSP1-2111 as a Brain Penetrant Group III Metabotropic Glutamate Receptor Orthosteric Agonist. |
Lundbeck Research Usa |
23947773 |
79 |
Dihydrothiazolopyridone derivatives as a novel family of positive allosteric modulators of the metabotropic glutamate 5 (mGlu5) receptor. |
Janssen Pharmaceutica |
22981332 |
58 |
Optimization of an ether series of mGlu5 positive allosteric modulators: molecular determinants of MPEP-site interaction crossover. |
Vanderbilt University Medical Center |
22148748 |
23 |
Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery. |
Vanderbilt University Medical Center |
22465637 |
48 |
4-(1-Phenyl-1H-pyrazol-4-yl)quinolines as novel, selective and brain penetrant metabotropic glutamate receptor 4 positive allosteric modulators. |
Lundbeck Research Usa |
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 |
21247167 |
57 |
Discovery, synthesis, and structure-activity relationship development of a series of N-(4-acetamido)phenylpicolinamides as positive allosteric modulators of metabotropic glutamate receptor 4 (mGlu(4)) with CNS exposure in rats. |
Vanderbilt University Medical Center |
19042134 |
30 |
Design, synthesis and biological evaluation of novel bicyclo[1.1.1]pentane-based omega-acidic amino acids as glutamate receptors ligands. |
Universit£ |
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 |
17725337 |
40 |
Synthesis, molecular modeling studies, and preliminary pharmacological characterization of all possible 2-(2'-sulfonocyclopropyl)glycine stereoisomers as conformationally constrained L-homocysteic acid analogs. |
Universit£ |
12109902 |
15 |
Common and selective molecular determinants involved in metabotopic glutamate receptor agonist activity. |
Parc Club Orsay Universit£ |
10893301 |
270 |
Ligands for glutamate receptors: design and therapeutic prospects. |
The Royal Danish School Of Pharmacy |
9572889 |
39 |
Synthesis and biology of the conformationally restricted ACPD analogue, 2-aminobicyclo[2.1.1]hexane-2,5-dicarboxylic acid-I, a potent mGluR agonist. |
Georgetown University Medical Center |
8759641 |
48 |
A new highly selective metabotropic excitatory amino acid agonist: 2-amino-4-(3-hydroxy-5-methylisoxazol-4-yl)butyric acid. |
Royal Danish School Of Pharmacy |
7738999 |
88 |
Metabotropic glutamate receptors: novel targets for drug development. |
Cns Research |
9873471 |
111 |
Synthesis and metabotropic glutamate receptor antagonist activity of N1-substituted analogs of 2R,4R-4-aminopyrrolidine-2,4-dicarboxylic acid. |
Eli Lilly |
22030026 |
13 |
Synthesis and SAR of a novel metabotropic glutamate receptor 4 (mGlu4) antagonist: unexpected 'molecular switch' from a closely related mGlu4 positive allosteric modulator. |
Vanderbilt University Medical Center |
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 |
21688779 |
84 |
Tricyclic thiazolopyrazole derivatives as metabotropic glutamate receptor 4 positive allosteric modulators. |
Lundbeck Research Usa |
19443219 |
39 |
Discovery and SAR of novel mGluR5 non-competitive antagonists not based on an MPEP chemotype. |
Vanderbilt University Medical Center |
21036612 |
10 |
1,2,3-triazolyl amino acids as AMPA receptor ligands. |
The University Of Adelaide |
20638290 |
9 |
A new metabotropic glutamate receptor agonist with in vivo anti-allodynic activity. |
The University Of Adelaide |
20667732 |
23 |
Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS). |
Vanderbilt University Medical Center |
20638279 |
46 |
An orally bioavailable positive allosteric modulator of the mGlu4 receptor with efficacy in an animal model of motor dysfunction. |
Evotec (Uk) |
19640716 |
12 |
Synthesis and SAR of a novel positive allosteric modulator (PAM) of the metabotropic glutamate receptor 4 (mGluR4). |
Vanderbilt University Medical Center |
19469556 |
47 |
Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). |
Vanderbilt University Medical Center |
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 |
19097893 |
8 |
Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4). Part II: Challenges in hit-to-lead. |
Vanderbilt University Medical Center |
17602546 |
20 |
Synthesis and biological evaluation of 1-amino-2-phosphonomethylcyclopropanecarboxylic acids, new group III metabotropic glutamate receptor agonists. |
University Paris Descartes |
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 |
16809035 |
15 |
Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists. |
Abbott Laboratories |
15582410 |
2 |
2,3-Ethylene- and 2,3-trimethylene-bridged analogues of the group III metabotropic glutamate receptor ligand 2-amino-4-phosphonobutanoic acid. |
University Of Minnesota |
10888329 |
22 |
Synthesis, molecular modeling and preliminary biological evaluation of 1-amino-3-phosphono-3-cyclopentene-1-carboxylic acid and 1-amino-3-phosphono-2-cyclopentene-1-carboxylic acid, two novel agonists of metabotropic glutamate receptors of group III. |
Università |
10866390 |
7 |
(+)-4-phosphonophenylglycine (PPG) a new group III selective metabotropic glutamate receptor agonist. |
Novartis Pharma |
10090786 |
33 |
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 for group II metabotropic glutamate receptors |
Eli Lilly |
9873635 |
67 |
2,3'-disubstituted-2-(2'-carboxycyclopropyl)glycines as potent and selective antagonists of metabotropic glutamate receptors. |
Eli Lilly |
9873392 |
6 |
Synthesis and preliminary evaluation of (S)-2-(4'-carboxycubyl)glycine, a new selective mGluR1 antagonist. |
Università |
9873391 |
15 |
Synthesis and pharmacology of N-alkylated derivatives of the excitotoxin ibotenic acid. |
Royal Danish School Of Pharmacy |
9871538 |
22 |
(2S,4S)-amino-4-(2,2-diphenylethyl)pentanedioic acid selective group 2 metabotropic glutamate receptor antagonist. |
Eli Lilly |
9301676 |
14 |
Synthesis and pharmacological characterization of aminocyclopentanetricarboxylic acids: new tools to discriminate between metabotropic glutamate receptor subtypes. |
Université |
8709120 |
17 |
(S)-(+)-2-(3'-carboxybicyclo[1.1.1]pentyl)-glycine, a structurally new group I metabotropic glutamate receptor antagonist. |
Università |
8667369 |
121 |
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. |
Università |
7562903 |
10 |
1-Aminoindan-1,5-dicarboxylic acid: a novel antagonist at phospholipase C-linked metabotropic glutamate receptors. |
Università |
29350927 |
102 |
Synthesis and Pharmacological Characterization of C4 |
TBA |
28902994 |
55 |
Discovery, Structure-Activity Relationship, and Antiparkinsonian Effect of a Potent and Brain-Penetrant Chemical Series of Positive Allosteric Modulators of Metabotropic Glutamate Receptor 4. |
Prexton Therapeutics |
9685236 |
100 |
Novel Nonnucleoside Inhibitors of HIV-1 Reverse Transcriptase. 8. 8-Aryloxymethyl- and 8-Arylthiomethyldipyridodiazepinones |
Boehringer Ingelheim Pharmaceuticals |
14622012 |
54 |
Multidrug resistance to HIV-1 protease inhibition requires cooperative coupling between distal mutations. |
The Johns Hopkins University |