ArticleJournal of medicinal chemistry2015
Discovery of a Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents.
Article in Journal of medicinal chemistry, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers.
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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.
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Who cites it
30 citing papers in PubMed.
- Discovery of VU6066098: A Selective and CNS-Penetrant mGluACS chemical neuroscience · 2026Article
- Article
- The Lateral Metalation of Isoxazolo[3,4-Molecules (Basel, Switzerland) · 2023Article
- Are mGluR2/3 Inhibitors Potential Compounds for Novel Antidepressants?Cellular and molecular neurobiology · 2023Review
- The role of thalamic group II mGlu receptors in health and disease.Neuronal signaling · 2022Review
- Metabotropic glutamate receptor 3 as a potential therapeutic target for psychiatric and neurological disorders.Pharmacology, biochemistry, and behavior · 2022Review
- Advances in translating mGluPharmacology, biochemistry, and behavior · 2022Review
- Allosteric Modulators of Metabotropic Glutamate Receptors as Novel Therapeutics for Neuropsychiatric Disease.Pharmacological reviews · 2022Review
- The effects of predator odor (TMT) exposure and mGluNeuropharmacology · 2022Article
- Discovery of "Molecular Switches" within a Series of mGluACS bio & med chem Au · 2021Article
- Frontal cortex genetic ablation of metabotropic glutamate receptor subtype 3 (mGluNeuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2021Article
- Activating mGluBiological psychiatry · 2021Article
- Targeting metabotropic glutamate receptors for the treatment of depression and other stress-related disorders.Neuropharmacology · 2021Review
- Exposure to the predator odor TMT induces early and late differential gene expression related to stress and excitatory synaptic function throughout the brain in male rats.Genes, brain, and behavior · 2020Article
- mGluNeuron · 2020Article
- Neurobiology of rapid-acting antidepressants: convergent effects on GluA1-synaptic function.Molecular psychiatry · 2019Review
- Metabotropic glutamate receptor subtype 3 gates acute stress-induced dysregulation of amygdalo-cortical function.Molecular psychiatry · 2019Article
- Neuropharmacological Insight from Allosteric Modulation of mGlu Receptors.Trends in pharmacological sciences · 2019Review
- Functional partnership between mGlu3 and mGlu5 metabotropic glutamate receptors in the central nervous system.Neuropharmacology · 2018Article
- Group II Metabotropic Glutamate Receptors: Role in Pain Mechanisms and Pain Modulation.Frontiers in molecular neuroscience · 2018Review
Corrections and comments
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Authors and funding
16 authors.
Funding
Abstract
Previous preclinical work has demonstrated the therapeutic potential of antagonists of the group II metabotropic glutamate receptors (mGlus). Still, compounds that are selective for the individual group II mGlus (mGlu2 and mGlu3) have been scarce. There remains a need for such compounds with the balance of properties suitable for convenient use in a wide array of rodent behavioral studies. We describe here the discovery of a selective mGlu3 NAM 106 (VU0650786) suitable for in vivo work. Compound 106 is a member of a series of 5-aryl-6,7-dihydropyrazolo[1,5-a]pyrazine-4(5H)-one compounds originally identified as a mGlu5 positive allosteric modulator (PAM) chemotype. Its suitability for use in rodent behavioral models has been established by extensive in vivo PK studies, and the behavioral experiments presented here with compound 106 represent the first examples in which an mGlu3 NAM has demonstrated efficacy in models where prior efficacy had previously been noted with nonselective group II antagonists.
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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.