ArticleBMC neuroscience2015
Constitutive activity of metabotropic glutamate receptor 7.
Article in BMC neuroscience, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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Who cites it
23 citing papers in PubMed, 34 citations in OpenAlex.
- Structural basis for modulation of group III mGlu receptors by transsynaptic interactions.Science advances · 2026Article
- Negative allosteric modulation of mGlu7 disrupts fear memory reconsolidation and glutamatergic signaling in rat and human brain tissue.Molecular psychiatry · 2026Article
- Overexpression of mGluMolecular neurobiology · 2025Article
- Metabotropic glutamate receptor homo- and heterodimers exhibit distinct responses to orthosteric and allosteric ligands.Molecular pharmacology · 2025Article
- Profiling the Impact of mGluACS chemical neuroscience · 2025Article
- Promiscuous involvement of metabotropic glutamate receptors in the storage ofPhilosophical transactions of the Royal Society of London. Series B, Biological sciences · 2024Article
- Therapeutic Potential for Metabotropic Glutamate Receptor 7 Modulators in Cognitive Disorders.Molecular pharmacology · 2024Review
- Signaling Specificity and Kinetics of the Human Metabotropic Glutamate Receptors.Molecular pharmacology · 2024Article
- Analysis of single nucleotide polymorphisms of the metabotropic glutamate receptors in a transgender population.Frontiers in endocrinology · 2024Article
- Differential Activity of Orthosteric Agonists and Allosteric Modulators at Metabotropic Glutamate Receptor 7.Molecular pharmacology · 2023Article
- GRM7 gene mutations and consequences for neurodevelopment.Pharmacology, biochemistry, and behavior · 2023Review
- Persistent challenges in the development of an mGluBioorganic & medicinal chemistry letters · 2023Article
- Development and profiling of mGluBioorganic & medicinal chemistry letters · 2022Article
- Subsynaptic mobility of presynaptic mGluR types is differentially regulated by intra- and extracellular interactions.Molecular biology of the cell · 2022Article
- Postmitotic Prox1 Expression Controls the Final Specification of Cortical VIP Interneuron Subtypes.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2021Article
- The G Protein-Coupled Glutamate Receptors as Novel Molecular Targets in Schizophrenia Treatment-A Narrative Review.Journal of clinical medicine · 2021Review
- Trans-Synaptic Regulation of Metabotropic Glutamate Receptors by Elfn Proteins in Health and Disease.Frontiers in neural circuits · 2021Article
- GRK2 Dictates a Functional Switch of the Peripheral Mu-Opioid Receptor.ACS chemical neuroscience · 2020Article
- Elfn1-Induced Constitutive Activation of mGluR7 Determines Frequency-Dependent Recruitment of Somatostatin Interneurons.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2019Article
- Progress toward allosteric ligands of metabotropic glutamate 7 (mGlu7) receptor: 2008-present.MedChemComm · 2019Review
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Authors and funding
1 author at 1 institution in 1 country.
Funding
Abstract
backgroundMetabotropic glutamate receptors (mGluRs) are class C G protein coupled receptors with widespread central nervous system expression. mGluR7 is a member of this family that has been implicated in numerous physiological and pathological processes, but the very low potency of mGluR7 for glutamate, its natural ligand, raise questions about the nature of its physiological role.
resultsHere, evidence is presented using heterologous expression in sympathetic neurons from the rat superior cervical ganglion (SCG) and modulation of the native SCG calcium currents as an assay for receptor signaling, that mGluR7 exhibits constitutive activity. This activity is detectable as basal calcium channel modulation in the absence of ligand that is not observed in untransfected cells or those transfected with other members of the mGluR family. Further, this basal channel modulation was reversibly inhibited with the mGluR7 inverse agonist MMPIP. Surprisingly, MMPIP did not strongly inhibit agonist-induced mGluR7 activation. Finally, the selective mGluR8 agonist (R,S)-PPG was also able to act as an inverse agonist at mGluR7.
conclusionsThese findings introduce a novel potential physiological role for mGluR7 in the nervous system, that of a constitutively active receptor, and thereby suggest a model in which mGluR7 signaling may be impactful without the need to invoke strong receptor activation by millimolar concentrations of extracellular glutamate. Constitutive activity of mGluR7 may be eliminated or reduced by the presence of other group III mGluRs, perhaps due to heterodimer formation. In addition, both MMPIP and PPG acted as inverse agonists at mGluR7, and agonists at mGluR8.
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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.