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Abbreviation : mGlu5
Long Form : metabotropic glutamate receptor 5
No. Year Title Co-occurring Abbreviation
2020 Differential contribution of metabotropic glutamate receptor 5 common allosteric binding site residues to biased allosteric agonism. PAMs
2020 Metabotropic glutamate receptor 5 in bulimia nervosa. ACC, BN, DVR, PET
2020 Metabotropic glutamate receptor subtype 5 (mGlu5) is necessary for estradiol mitigation of light-induced anxiety behavior in female rats. ---
2020 mGlu5 in GABAergic neurons modulates spontaneous and psychostimulant-induced locomotor activity. LTD, MPEP, OFA
2020 Probe dependence and biased potentiation of metabotropic glutamate receptor 5 is mediated by differential ligand interactions in the common allosteric binding site. 7TM, PAM
2020 The cognitive cost of reducing relapse to cocaine-seeking with mGlu5 allosteric modulators. CDPPB, CUD, DMS, MTEP
2020 The infralimbic cortex and mGlu5 mediate the effects of chronic intermittent ethanol exposure on fear learning and memory. AUD, CIE, IfL, PTSD
2020 The metabotropic glutamate receptor 5 negative allosteric modulator fenobam: pharmacokinetics, side effects, and analgesic effects in healthy human subjects. ---
2019 Estradiol-Induced Potentiation of Dopamine Release in Dorsal Striatum Following Amphetamine Administration Requires Estradiol Receptors and mGlu5. DA, DLS, MPEP
10  2019 Evaluation of Amides, Carbamates, Sulfonamides, and Ureas of 4-Prop-2-ynylidenecycloalkylamine as Potent, Selective, and Bioavailable Negative Allosteric Modulators of Metabotropic Glutamate Receptor 5. NAMs
11  2019 Identification of monellin as the first naturally derived proteinaceous allosteric agonist of metabotropic glutamate receptor 5. GPCRs
12  2019 In Vitro to in Vivo Translation of Allosteric Modulator Concentration-Effect Relationships: Implications for Drug Discovery. PAMs
13  2019 Increased Alcohol-Drinking Induced by Manipulations of mGlu5 Phosphorylation within the Bed Nucleus of the Stria Terminalis. BNST, ERK
14  2019 Kinetic and system bias as drivers of metabotropic glutamate receptor 5 allosteric modulator pharmacology. NAMs
15  2019 Mechanisms underlying the efficacy of exercise as an intervention for cocaine relapse: a focus on mGlu5 in the dorsal medial prefrontal cortex. dmPFC
16  2019 Metabotropic glutamate receptor 5 (mGlu5 )-positive allosteric modulators differentially induce or potentiate desensitization of mGlu5 signaling in recombinant cells and neurons. DHPG
17  2019 Numb deficiency causes impaired trafficking of mGlu5 in neurons and autistic-like behaviors. mGlu1
18  2019 Pathophysiological clues to therapeutic applications of glutamate mGlu5 receptor antagonists in levodopa-induced dyskinesia. LID, MAPK, PD, REM
19  2019 Radiation dosimetry of [18F]-PSS232-a PET radioligand for imaging mGlu5 receptors in humans. ---
20  2019 Structure-Based Optimization Strategies for G Protein-Coupled Receptor (GPCR) Allosteric Modulators: A Case Study from Analyses of New Metabotropic Glutamate Receptor 5 (mGlu5) X-ray Structures. GPCR, NAM
21  2019 The role of water and protein flexibility in the structure-based virtual screening of allosteric GPCR modulators: an mGlu5 receptor case study. GPCRs
22  2018 A first-in-man PET study of [18F]PSS232, a fluorinated ABP688 derivative for imaging metabotropic glutamate receptor subtype 5. DVR
23  2018 Activated CaMKIIalpha Binds to the mGlu5 Metabotropic Glutamate Receptor and Modulates Calcium Mobilization. CaMKII, CTD
24  2018 Alcohol Addiction- Metabotropic Glutamate Receptor Subtype 5 and its Ligands: How They All Come Together? MTEP, PKCepsilon
25  2018 Altered expression of schizophrenia-related genes in mice lacking mGlu5 receptors. KO
26  2018 Automated cGMP-compliant radiosynthesis of [18 F]-(E)-PSS232 for brain PET imaging of metabotropic glutamate receptor subtype 5. DMSO, HPLC
27  2018 Biased agonism and allosteric modulation of metabotropic glutamate receptor 5. ---
28  2018 Downregulation of metabotropic glutamate receptor 5 inhibits hepatoma development in a neurotoxin rotenone-induced Parkinson's disease model. CHPG, DEN, MPEP, NAC, PD, ROS
29  2018 Exploring the Binding Mechanism of Metabotropic Glutamate Receptor 5 Negative Allosteric Modulators in Clinical Trials by Molecular Dynamics Simulations. MD, NAMs, TM
30  2018 Lower Limbic Metabotropic Glutamate Receptor 5 Availability in Alcohol Dependence. 18F-FPEB
31  2018 mGlu5 Receptor Blockade Within the Nucleus Accumbens Shell Reduces Behavioral Indices of Alcohol Withdrawal-Induced Anxiety in Mice. ---
32  2018 mGlu5-dependent modulation of anxiety during early withdrawal from binge-drinking in adult and adolescent male mice. AcbSh
33  2018 Results and evaluation of a first-in-human study of RG7342, an mGlu5 positive allosteric modulator, utilizing Bayesian adaptive methods. DLEs, MTD, PAM
34  2018 The influence of AMN082, metabotropic glutamate receptor 7 (mGlu7) allosteric agonist on the acute and chronic antinociceptive effects of morphine in the tail-immersion test in mice: Comparison with mGlu5 and mGlu2/3 ligands. mGlu7, NMDA
35  2018 Touchscreen testing reveals clinically relevant cognitive abnormalities in a mouse model of schizophrenia lacking metabotropic glutamate receptor 5. KO, TUNL
36  2017 A Phase I randomized clinical trial testing the safety, tolerability and preliminary pharmacokinetics of the mGluR5 negative allosteric modulator GET 73 following single and repeated doses in healthy volunteers. AEs, PK
37  2017 beta-Arrestin2 Couples Metabotropic Glutamate Receptor 5 to Neuronal Protein Synthesis and Is a Potential Target to Treat Fragile X. FX
38  2017 Biased allosteric agonism and modulation of metabotropic glutamate receptor 5: Implications for optimizing preclinical neuroscience drug discovery. ---
39  2017 Blocking metabotropic glutamate receptor subtype 5 relieves maladaptive chronic stress consequences. ---
40  2017 Chronic oral administration of MPEP, an antagonist of mGlu5 receptor, during gestation and lactation alters mGlu5 and A2A receptors in maternal and neonatal brain. A2AR, mGlu receptors, MPEP, PLC
41  2017 Discovery of 4-amino-3-arylsulfoquinolines, a novel non-acetylenic chemotype of metabotropic glutamate 5 (mGlu5) receptor negative allosteric modulators. ---
42  2017 Homer1 Scaffold Proteins Govern Ca2+ Dynamics in Normal and Reactive Astrocytes. ER
43  2017 Illuminating Phenylazopyridines To Photoswitch Metabotropic Glutamate Receptors: From the Flask to the Animals. NAM
44  2017 Integrated In Silico Fragment-Based Drug Design: Case Study with Allosteric Modulators on Metabotropic Glutamate Receptor 5. GPCRs, RECAP
45  2017 Pharmacological enhancement of mGlu5 receptors rescues behavioral deficits in SHANK3 knock-out mice. ASD, ID, PMS, PSD
46  2017 Positional isomers of bispyridine benzene derivatives induce efficacy changes on mGlu5 negative allosteric modulation. ---
47  2017 The activation of metabotropic glutamate 5 receptors in the rat ventral tegmental area increases dopamine extracellular levels. CHPG, DA, VTA
48  2016 An mGlu5-Positive Allosteric Modulator Rescues the Neuroplasticity Deficits in a Genetic Model of NMDA Receptor Hypofunction in Schizophrenia. NMDAR, SCZ, SR
49  2016 Clickable Photoaffinity Ligands for Metabotropic Glutamate Receptor 5 Based on Select Acetylenic Negative Allosteric Modulators. GPCRs, NAM
50  2016 Glutamate Delta-1 Receptor Regulates Metabotropic Glutamate Receptor 5 Signaling in the Hippocampus. DHPG, GluD1, mTOR
51  2016 Metabotropic glutamate receptor subtype 5: molecular pharmacology, allosteric modulation and stimulus bias. ---
52  2016 mGlu5 positive allosteric modulation normalizes synaptic plasticity defects and motor phenotypes in a mouse model of Rett syndrome. PAM, PSDSP, RS
53  2016 Multiple D2 heteroreceptor complexes: new targets for treatment of schizophrenia. 5-HT2A, DA, GABA, GPCRs, NMDA
54  2016 Partial mGlu₅ Negative Allosteric Modulators Attenuate Cocaine-Mediated Behaviors and Lack Psychotomimetic-Like Effects. NAMs
55  2016 Perirhinal Cortex mGlu5 Receptor Activation Reduces Relapse to Methamphetamine Seeking by Restoring Novelty Salience. METH, PAM
56  2016 The effects of acute ethanol administration on ethanol withdrawal-induced anxiety-like syndrome in rats: A biochemical study. EW, PKC
57  2016 VU0477573: Partial Negative Allosteric Modulator of the Subtype 5 Metabotropic Glutamate Receptor with In Vivo Efficacy. CNS, IP, NAMs
58  2015 Acyl dihydropyrazolo[1,5-a]pyrimidinones as metabotropic glutamate receptor 5 positive allosteric modulators. AHL, PAMs
59  2015 Basimglurant for treatment of major depressive disorder: a novel negative allosteric modulator of metabotropic glutamate receptor 5. MPEP, MTEP, NAM
60  2015 Biased mGlu5-Positive Allosteric Modulators Provide In Vivo Efficacy without Potentiating mGlu5 Modulation of NMDAR Currents. NMDAR, PAMs
61  2015 Discovery and SAR of novel series of imidazopyrimidinones and dihydroimidazopyrimidinones as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5). DMPK, PAMs
62  2015 Discovery of VU0409551/JNJ-46778212: An mGlu5 Positive Allosteric Modulator Clinical Candidate Targeting Schizophrenia. PAMs
63  2015 Environmental Enrichment Ameliorates Behavioral Impairments Modeling Schizophrenia in Mice Lacking Metabotropic Glutamate Receptor 5. EE, KO, PPI
64  2015 Extinction of a cocaine-taking context that protects against drug-primed reinstatement is dependent on the metabotropic glutamate 5 receptor. ---
65  2015 Identification and optimisation of a series of tetrahydrobenzotriazoles as metabotropic glutamate receptor 5-selective positive allosteric modulators that improve performance in a preclinical model of cognition. NOR, PAMs
66  2015 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. NAMs
67  2015 Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases. FXS, NAMs
68  2015 Pharmacology of basimglurant (RO4917523, RG7090), a unique metabotropic glutamate receptor 5 negative allosteric modulator in clinical development for depression. MDD
69  2015 Preclinical evaluation and test-retest studies of [(18)F]PSS232, a novel radioligand for targeting metabotropic glutamate receptor 5 (mGlu5). ---
70  2015 Relationship between in vivo receptor occupancy and efficacy of metabotropic glutamate receptor subtype 5 allosteric modulators with different in vitro binding profiles. PET
71  2015 Spatial Learning Requires mGlu5 Signalling in the Dorsal Hippocampus. ---
72  2014 Chronic metabotropic glutamate receptor 5 inhibition corrects local alterations of brain activity and improves cognitive performance in fragile X mice. FXS, KO, WT
73  2014 Discovery and SAR of a novel series of metabotropic glutamate receptor 5 positive allosteric modulators with high ligand efficiency. HBA, PAMs
74  2014 Identification of specific ligand-receptor interactions that govern binding and cooperativity of diverse modulators to a common metabotropic glutamate receptor 5 allosteric site. SAR
75  2014 Interaction of adenosine receptors with other receptors from therapeutic perspective in Parkinson's disease. L-DOPA, PD
76  2014 SAR studies on mGlu5 receptor positive allosteric modulators (2003- 2013). ATD, PAM, SAR
77  2014 Tetrahydronaphthyridine and dihydronaphthyridinone ethers as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu₅). PAMs
78  2014 The effect of the mGlu5 negative allosteric modulator MTEP and NMDA receptor partial agonist D-cycloserine on Pavlovian conditioned fear. DCS, MTEP, NMDA
79  2014 Therapeutic potential of targeting glutamate receptors in Parkinson's disease. ---
80  2013 A novel metabotropic glutamate receptor 5 positive allosteric modulator acts at a unique site and confers stimulus bias to mGlu5 signaling. CNS, LTD, LTP, PAMs
81  2013 Biotransformation of a novel positive allosteric modulator of metabotropic glutamate receptor subtype 5 contributes to seizure-like adverse events in rats involving a receptor agonism-dependent mechanism. PAMs
82  2013 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. NAMs
83  2013 Effects of a metabotropic glutamate receptor 5 positive allosteric modulator, CDPPB, on spatial learning task performance in rodents. ---
84  2013 Exploration of allosteric agonism structure-activity relationships within an acetylene series of metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs): discovery of 5-((3-fluorophenyl)ethynyl)-N-(3-methyloxetan-3-yl)picolinamide (ML254). ago-PAMs, PAMs
85  2013 Metabotropic glutamate receptor 5-negative allosteric modulators for the treatment of psychiatric and neurological disorders (2009-July 2013). ---
86  2013 mGlu5 negative allosteric modulators: a patent review (2010-2012). FXS, GERD, NAMs, PD-LID
87  2013 N-aryl piperazine metabotropic glutamate receptor 5 positive allosteric modulators possess efficacy in preclinical models of NMDA hypofunction and cognitive enhancement. DPFE, NMDA, PAMs
88  2013 Substituted 1-Phenyl-3-(pyridin-2-yl)urea negative allosteric modulators of mGlu5: discovery of a new tool compound VU0463841 with activity in rat models of cocaine addiction. CNS, NAM
89  2013 The metabotropic glutamate 5 receptor modulates extinction and reinstatement of methamphetamine-seeking in mice. KO, METH
90  2013 Unique signaling profiles of positive allosteric modulators of metabotropic glutamate receptor subtype 5 determine differences in in vivo activity. PAMs
91  2012 Could MDMA Promote Stemness Characteristics in Mouse Embryonic Stem Cells via mGlu5 Metabotropic Glutamate Receptors? MDMA, mESCs, RT-PCR
92  2012 Extracellular cysteine (Cys)/cystine (CySS) redox regulates metabotropic glutamate receptor 5 activity. AMS, Cys, ERK, HEK293, iNOS, MAPK, MPEP, PD, ROS, SAA
93  2012 mGlu5 Receptor Functional Interactions and Addiction. GPCR
94  2012 The suppressive effect of metabotropic glutamate receptor 5 (mGlu5) inhibition on hepatocarcinogenesis. CNS, DHPG, ERK, HCC, MAPK, mGlus, MPEP
95  2011 CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor. CTEP, MPEP
96  2011 Discovery of novel positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5). ---
97  2011 Functional interaction of mGlu5 and NMDA receptors in aversive learning in rats. CDPPB
98  2010 Novel heterocyclic compounds as mGlu5 antagonists: WO2009015897. NAMs
99  2010 Reduction of L-DOPA-induced dyskinesia by the selective metabotropic glutamate receptor 5 antagonist 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine in the 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-lesioned macaque model of Parkinson's disease. LID, MPTP, MTEP
100  2009 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. ---