ReviewMolecules (Basel, Switzerland)2011
Positive allosteric modulators of type 5 metabotropic glutamate receptors (mGluR5) and their therapeutic potential for the treatment of CNS disorders.
Review in Molecules (Basel, Switzerland), 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 44 papers.
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Who cites it
44 citing papers in PubMed, 76 citations in OpenAlex.
- Amygdala-hippocampus circuit regulates stress coping via mGluR5-dependent BDNF signaling.Molecules and cells · 2026Article
- mGluR5 as a Potential Orchestrator of Astrocyte Interactions in Neurological Disorders.Neural plasticity · 2025Review
- Exploring the material basis and molecular targets of Changma Xifeng tablet in treating Tourette syndrome: an integrative approach of network pharmacology and miRNA analysis.Metabolic brain disease · 2024Article
- Regulation of neuronal circHomer1 biogenesis by PKA/CREB/ERK-mediated pathways and effects of glutamate and dopamine receptor blockade.Research square · 2024Article
- Mesocorticolimbic function in cocaine polydrug users: A multimodal study of drug cue reactivity and cognitive regulation.Addiction biology · 2024Article
- The Evolving Landscape of Therapeutics for Epilepsy in Tuberous Sclerosis Complex.Biomedicines · 2023Review
- Differences in Quantification of the Metabotropic Glutamate Receptor 5 Across Bipolar Disorder and Major Depressive Disorder.Biological psychiatry · 2023Article
- Role of mGlu5 in Persistent Forms of Hippocampal Synaptic Plasticity and the Encoding of Spatial Experience.Cells · 2022Review
- Transcriptome Profiling of the Dorsomedial Prefrontal Cortex in Suicide Victims.International journal of molecular sciences · 2022Article
- Modulation of mGlu5 improves sensorimotor gating deficits in rats neonatally treated with quinpirole through changes in dopamine D2 signaling.Pharmacology, biochemistry, and behavior · 2021Article
- Synthesis, Biodistribution, and Radiation Dosimetry of a Novel mGluR5 Radioligand:ACS chemical neuroscience · 2020Article
- Recovery of Decreased Metabotropic Glutamate Receptor 5 Availability in Abstinent Alcohol-Dependent Patients.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2020Article
- Lrrc7 mutant mice model developmental emotional dysregulation that can be alleviated by mGluR5 allosteric modulation.Translational psychiatry · 2019Article
- Metabotropic Glutamate Receptor Subtype 5 in Alcohol-Induced Negative Affect.Brain sciences · 2019Review
- Biphasic Modulation of NMDA Receptor Function by Metabotropic Glutamate Receptors.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2018Article
- Selective Blockade of the Metabotropic Glutamate Receptor mGluR5 Protects Mouse Livers in In Vitro and Ex Vivo Models of Ischemia Reperfusion Injury.International journal of molecular sciences · 2018Article
- Glutamatergic regulation of cognition and functional brain connectivity: insights from pharmacological, genetic and translational schizophrenia research.British journal of pharmacology · 2017Review
- Acute inhibition of mGluR5 disrupts behavioral flexibility.Neurobiology of learning and memory · 2016Article
- Spatial Learning Requires mGlu5 Signalling in the Dorsal Hippocampus.Neurochemical research · 2015Article
- The mGluR5 positive allosteric modulator CDPPB inhibits SO₂-induced protein radical formation and mitochondrial dysfunction through activation of Akt in mouse hippocampal HT22 cells.Cellular and molecular neurobiology · 2015Article
Corrections and comments
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
Abstract
Studies utilizing selective pharmacological antagonists or targeted gene deletion have demonstrated that type 5 metabotropic glutamate receptors (mGluR5) are critical mediators and potential therapeutic targets for the treatment of numerous disorders of the central nervous system (CNS), including depression, anxiety, drug addiction, chronic pain, Fragile X syndrome, Parkinson's disease, and gastroesophageal reflux disease. However, in recent years, the development of positive allosteric modulators (PAMs) of the mGluR5 receptor have revealed that allosteric activation of this receptor may also be of potential therapeutic benefit for the treatment of other CNS disorders, including schizophrenia, cognitive deficits associated with chronic drug use, and deficits in extinction learning. Here we summarize the discovery and characterization of various mGluR5 PAMs, with an emphasis on those that are systemically active. We will also review animal studies showing that these molecules have potential efficacy as novel antipsychotic agents. Finally, we will summarize findings that suggest that mGluR5 PAMs have pro-cognitive effects such as the ability to enhance synaptic plasticity, improve performance in various learning and memory tasks, including extinction of drug-seeking behavior, and reverse cognitive deficits produced by chronic drug use.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.