ArticleACS chemical neuroscience2014
Identification of positive allosteric modulators VU0155094 (ML397) and VU0422288 (ML396) reveals new insights into the biology of metabotropic glutamate receptor 7.
Article in ACS chemical neuroscience, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 40 papers, 1 of them a synthesis that pooled it.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
40 citing papers in PubMed, 1 synthesis or guideline pooled it, 65 citations in OpenAlex.
- Comprehensive gene- and pathway-based analysis of depressive symptoms in older adults.Journal of Alzheimer's disease : JAD · 2015Pooled it
- Structural basis for modulation of group III mGlu receptors by transsynaptic interactions.Science advances · 2026Article
- Discovery of VU6081679, a Novel Positive Allosteric Modulator of Metabotropic Glutamate Receptor 8 with Efficacy in a Preclinical Model of Parkinson's Disease.ACS chemical neuroscience · 2026Article
- Molecular pharmacology of mGluMolecular pharmacology · 2026Article
- Profiling metabotropic glutamate receptor 7 expression in Rett syndrome: consequences for pharmacotherapy.Neuroscience · 2026Article
- Overexpression of mGluMolecular neurobiology · 2025Article
- Targeting mGluR7 in Parkinson's disease: a novel approach to neuroprotection and synaptic therapies.Inflammopharmacology · 2025Review
- Profiling the Impact of mGluACS chemical neuroscience · 2025Article
- Potentiation of group III metabotropic glutamate receptors positively affects neurophysiological features in a mouse model of Rett syndrome.The Journal of pharmacology and experimental therapeutics · 2025Article
- Therapeutic Potential for Metabotropic Glutamate Receptor 7 Modulators in Cognitive Disorders.Molecular pharmacology · 2024Review
- OXTR polymorphisms associated with severity and treatment responses of schizophrenia.Schizophrenia (Heidelberg, Germany) · 2024Article
- Differential Activity of Orthosteric Agonists and Allosteric Modulators at Metabotropic Glutamate Receptor 7.Molecular pharmacology · 2023Article
- Pharmacological Modulation of Excitotoxicity through the Combined Use of NMDA Receptor Inhibition and Group III mGlu Activation Reduces TMT-Induced Neurodegeneration in the Rat Hippocampus.International journal of molecular sciences · 2023Article
- Discovery ofACS medicinal chemistry letters · 2023Article
- GRM7 gene mutations and consequences for neurodevelopment.Pharmacology, biochemistry, and behavior · 2023Review
- The Role of Glutamatergic Gene Polymorphisms in the Clinical Phenotypes of Schizophrenia.Genes · 2023Article
- Design and Synthesis of New Quinazolin-4-one Derivatives with Negative mGluInternational journal of molecular sciences · 2023Article
- Persistent challenges in the development of an mGluBioorganic & medicinal chemistry letters · 2023Article
- New 1,2,4-oxadiazole derivatives with positive mGluJournal of enzyme inhibition and medicinal chemistry · 2022Article
- Development and profiling of mGluBioorganic & medicinal chemistry letters · 2022Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
23 authors at 3 institutions in 2 countries.
Funding
Abstract
Metabotropic glutamate receptor 7 (mGlu7) is a member of the group III mGlu receptors (mGlus), encompassed by mGlu4, mGlu6, mGlu7, and mGlu8. mGlu7 is highly expressed in the presynaptic active zones of both excitatory and inhibitory synapses, and activation of the receptor regulates the release of both glutamate and GABA. mGlu7 is thought to be a relevant therapeutic target for a number of neurological and psychiatric disorders, and polymorphisms in the GRM7 gene have been linked to autism, depression, ADHD, and schizophrenia. Here we report two new pan-group III mGlu positive allosteric modulators, VU0155094 and VU0422288, which show differential activity at the various group III mGlus. Additionally, both compounds show probe dependence when assessed in the presence of distinct orthosteric agonists. By pairing studies of these nonselective compounds with a synapse in the hippocampus that expresses only mGlu7, we have validated activity of these compounds in a native tissue setting. These studies provide proof-of-concept evidence that mGlu7 activity can be modulated by positive allosteric modulation, paving the way for future therapeutics development.
Indexed as
Identifiers
What OpenQuestion holds
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.