ADX71743, a Potent and Selective Negative Allosteric Modulator of Metabotropic Glutamate Receptor 7: In Vitro and In Vivo Characterization

No abstract is available for this paper.

• Publication year

  2013

• Venue

  Journal of Pharmacology and Experimental Therapeutics

• Publication date

  2013-03-01

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1124/jpet.112.200915PMID 23257312
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Metabotropic Glutamate Receptors

  2015cited by this paper
• Towards a glutamate hypothesis of depression: an emerging frontier of neuropsychopharmacology for mood disorders.

  2012cited by this paper
• The Metabotropic Glutamate Receptor 7 Allosteric Modulator AMN082: A Monoaminergic Agent in Disguise?

  2011cited by this paper
• Characterization of an mGluR2/3 Negative Allosteric Modulator in Rodent Models of Depression

  2011influential reference
• Effects of a novel metabotropic glutamate receptor 7 negative allosteric modulator, 6-(4-methoxyphenyl)-5-methyl-3-pyridin-4-ylisoxazonolo[4,5-c]pyridin-4(5H)-one (MMPIP), on the central nervous system in rodents.

  2010cited by this paper
• Context-Dependent Pharmacology Exhibited by Negative Allosteric Modulators of Metabotropic Glutamate Receptor 7

  2010cited by this paper
• Isoxazolopyridone derivatives as allosteric metabotropic glutamate receptor 7 antagonists.

  2010cited by this paper
• Conditioned avoidance response in the development of new antipsychotics.

  2010cited by this paper
• Metabotropic glutamate receptor 7: at the interface of cognition and emotion.

  2010cited by this paper
• Marble burying reflects a repetitive and perseverative behavior more than novelty-induced anxiety

  2009cited by this paper
• Association study of polymorphisms in the group III metabotropic glutamate receptor genes, GRM4 and GRM7, with schizophrenia.

  2009cited by this paper
• A family-based association study of DNA sequence variants in GRM7 with schizophrenia in an Indonesian population.

  2009cited by this paper
• Gestational methylazoxymethanol acetate administration: a developmental disruption model of schizophrenia.

  2009cited by this paper
• Group III mGluR7 and mGluR8 in the amygdala differentially modulate nocifensive and affective pain behaviors.

  2008cited by this paper
• Selective activation of metabotropic G-protein-coupled glutamate 7 receptor elicits anxiolytic-like effects in mice by modulating GABAergic neurotransmission

  2008cited by this paper
• A polymorphism of the metabotropic glutamate receptor mGluR7 (GRM7) gene is associated with schizophrenia.

  2008cited by this paper
• In Vitro Pharmacological Characterization of Novel Isoxazolopyridone Derivatives as Allosteric Metabotropic Glutamate Receptor 7 Antagonists

  2007cited by this paper
• Activation of the mGlu7 receptor elicits antidepressant-like effects in mice

  2007cited by this paper
• mGluR7 undergoes rapid internalization in response to activation by the allosteric agonist AMN082.

  2007influential reference
• A combined marble burying-locomotor activity test in mice: a practical screening test with sensitivity to different classes of anxiolytics and antidepressants.

  2006cited by this paper
• Concomitant Deficits in Working Memory and Fear Extinction Are Functionally Dissociated from Reduced Anxiety in Metabotropic Glutamate Receptor 7-Deficient Mice

  2006influential reference
• Metabotropic Glutamate Receptor Subtype 7 Ablation Causes Dysregulation of the HPA Axis and Increases Hippocampal BDNF Protein Levels: Implications for Stress-Related Psychiatric Disorders

  2006influential reference
• mGluR7's lucky number.

  2006cited by this paper
• Metabotropic glutamate receptors

  2006cited by this paper
• The Flinders Sensitive Line rat: a selectively bred putative animal model of depression.

  2005cited by this paper
• A selective metabotropic glutamate receptor 7 agonist: activation of receptor signaling via an allosteric site modulates stress parameters in vivo.

  2005influential reference
• Metabotropic glutamate receptors as novel targets for anxiety and stress disorders

  2005cited by this paper
• Behavioral, neurochemical, and electrophysiological characterization of a genetic mouse model of depression

  2003cited by this paper
• Animal behavior models of the mechanisms underlying antipsychotic atypicality.

  2003cited by this paper
• Antidepressant and anxiolytic‐like effects in mice lacking the group III metabotropic glutamate receptor mGluR7

  2003cited by this paper
• Preclinical pharmacology of mGlu2/3 receptor agonists: novel agents for schizophrenia?

  2002cited by this paper
• The role of amygdala glutamate receptors in fear learning, fear-potentiated startle, and extinction.

  2002cited by this paper
• Increased Seizure Susceptibility in Mice Lacking Metabotropic Glutamate Receptor 7

  2001cited by this paper
• Metabotropic Glutamate Receptor Subtype 7 Ablation Causes Deficit in Fear Response and Conditioned Taste Aversion

  1999cited by this paper
• Selectivity of action of typical and atypical anti-psychotic drugs as antagonists of the behavioral effects of 1-[2,5-dimethoxy-4-iodophenyl]-2-aminopropane (DOI).

  1999cited by this paper
• LY341495 is a nanomolar potent and selective antagonist of group II metabotropic glutamate receptors.

  1998cited by this paper
• Immunohistochemical localization of metabotropic glutamate receptors, mGluR7a and mGluR7b, in the central nervous system of the adult rat and mouse: A light and electron microscopic study

  1998influential reference
• Reversal of phencyclidine effects by a group II metabotropic glutamate receptor agonist in rats.

  1998cited by this paper
• A novel splice variant of a metabotropic glutamate receptor, human mGluR7b.

  1997cited by this paper
• Measurement and Analysis of Unbound Drug Concentrations

  1996cited by this paper
• Molecular characterization of a new metabotropic glutamate receptor mGluR7 coupled to inhibitory cyclic AMP signal transduction.

  1994cited by this paper
• Treatment of schizophrenia: a clinical and preclinical evaluation of neuroleptic drugs.

  1993cited by this paper
• Ethologically-based animal models of anxiety disorders.

  1990cited by this paper
• Measurement and analysis.

  1988cited by this paper
• Validation of open:closed arm entries in an elevated plus-maze as a measure of anxiety in the rat.

  1985cited by this paper

• Profiling metabotropic glutamate receptor 7 expression in Rett syndrome: consequences for pharmacotherapy

  2025cites this paper
• Negative allosteric modulation of mGlu7 disrupts fear memory reconsolidation and glutamatergic signaling in rat and human brain tissue

  2025influential citation
• Update on mGlu4 modulator patents: 2017 to present

  2025cites this paper
• Metabotropic glutamate receptors in GtoPdb v.2025.3

  2025cites this paper
• Profiling the Impact of mGlu7/Elfn1 Protein Interactions on the Pharmacology of mGlu7 Allosteric Modulators

  2025cites this paper
• Therapeutic Potential for Metabotropic Glutamate Receptor 7 Modulators in Cognitive Disorders

  2024cites this paper
• Novel Inhibitory Site Revealed by XAP044 Mode of Action on the Metabotropic Glutamate 7 Receptor Venus Flytrap Domain.

  2024cites this paper
• mGluR7: the new player protecting the central nervous system.

  2024cites this paper
• mGlu4R, mGlu7R, and mGlu8R allosteric modulation for treating acute and chronic neurodegenerative disorders

  2024cites this paper
• Metabotropic glutamate receptor function and regulation of sleep-wake cycles.

  2023cites this paper
• Discovery of CVN636: A Highly Potent, Selective, and CNS Penetrant mGluR7 Allosteric Agonist.

  2023cites this paper
• Metabotropic glutamate receptors and cognition: From underlying plasticity and neuroprotection to cognitive disorders and therapeutic targets.

  2023cites this paper
• Design and Synthesis of New Quinazolin-4-one Derivatives with Negative mGlu7 Receptor Modulation Activity and Antipsychotic-Like Properties

  2023influential citation
• Potential of olfactory neuroepithelial cells as a model to study schizophrenia: A focus on GPCRs (Review)

  2023cites this paper
• Targeting mGluR group III for the treatment of neurodegenerative diseases.

  2023cites this paper
• A sign-inverted receptive field of inhibitory interneurons provides a pathway for ON-OFF interactions in the retina

  2023cites this paper
• Anxiolytic-like effects of an mGluR 5 antagonist and a mGluR 2/3 agonist, and antidepressant-like effects of an mGluR 7 agonist in the chick social separation stress test, a dual-drug screening model of treatment-resistant depression.

  2023cites this paper
• Metabotropic glutamate receptors in GtoPdb v.2023.1

  2023cites this paper
• Differential Activity of Orthosteric Agonists and Allosteric Modulators at Metabotropic Glutamate Receptor 7

  2023cites this paper
• GRM7 gene mutations and consequences for neurodevelopment.

  2023cites this paper
• Metabotropic Glutamate Receptors As Emerging Targets for the Treatment of Schizophrenia

  2022cites this paper
• Efficacy of VMAT2 inhibition and synergy with antipsychotics in animal models of schizophrenia

  2022influential citation
• Differential activity of mGlu7 allosteric modulators provides evidence for mGlu7/8 heterodimers at hippocampal Schaffer collateral-CA1 synapses

  2022cites this paper
• Clinical investigations of compounds targeting metabotropic glutamate receptors.

  2022cites this paper
• Development and profiling of mGlu7 NAMs with a range of saturable inhibition of agonist responses in vitro.

  2022cites this paper
• The mGlu7 receptor in schizophrenia - An update and future perspectives.

  2022cites this paper
• Hearing loss drug discovery and medicinal chemistry: Current status, challenges, and opportunities.

  2022cites this paper
• Allosteric Modulators of Metabotropic Glutamate Receptors as Novel Therapeutics for Neuropsychiatric Disease

  2022cites this paper
• Blocking Metabotropic Glutamate Receptor Subtype 7 via the Venus Flytrap Domain Promotes a Chronic Stress-Resilient Phenotype in Mice

  2022cites this paper
• Efficacy of Vesicular Monoamine Transporter 2 Inhibition and Synergy with Antipsychotics in Animal Models of Schizophrenia

  2022influential citation
• The Role of G Protein-Coupled Receptors (GPCRs) and Calcium Signaling in Schizophrenia. Focus on GPCRs Activated by Neurotransmitters and Chemokines

  2021cites this paper
• New 1,2,4-oxadiazole derivatives with positive mGlu4 receptor modulation activity and antipsychotic-like properties

  2021cites this paper
• Metabotropic glutamate receptors in GtoPdb v.2021.3

  2021cites this paper
• Targeting metabotropic glutamate receptors for the treatment of depression and other stress-related disorders.

  2021cites this paper
• The G Protein-Coupled Glutamate Receptors as Novel Molecular Targets in Schizophrenia Treatment—A Narrative Review

  2021cites this paper
• Synthesis and SAR of a series of mGlu7 NAMs based on an ethyl-8-methoxy-4-(4-phenylpiperazin-1-yl)quinoline carboxylate core.

  2020cites this paper
• Allosteric modulators targeting GPCRs

  2020cites this paper
• Discovery of VU6027459: A First-in-Class Selective and CNS Penetrant mGlu7 Positive Allosteric Modulator Tool Compound.

  2020cites this paper
• Phenotypic profiling of mGlu7 knockout mice reveals new implications for neurodevelopmental disorders

  2020cites this paper
• Conformational pathway provides unique sensitivity to a synaptic mGluR

  2019cites this paper
• Depression and schizophrenia viewed from the perspective of amino acidergic neurotransmission: Antipodes of psychiatric disorders

  2019cites this paper
• Discovery of an Orally Bioavailable and Central Nervous System (CNS) Penetrant mGlu7 Negative Allosteric Modulator (NAM) in Vivo Tool Compound: N-(2-(1 H-1,2,4-triazol-1-yl)-5-(trifluoromethoxy)phenyl)-4-(cyclopropylmethoxy)-3-methoxybenzamide (VU6012962).

  2019cites this paper
• Role of Metabotropic Glutamate Receptors in Neurological Disorders

  2019cites this paper
• Neuropharmacological Insight from Allosteric Modulation of mGlu Receptors.

  2019cites this paper
• Progress toward allosteric ligands of metabotropic glutamate 7 (mGlu7) receptor: 2008-present.

  2019cites this paper
• The Role of Metabotropic Glutamate Receptors in Social Behavior in Rodents

  2019influential citation
• Surveying heterocycles as amide bioisosteres within a series of mGlu7 NAMs: Discovery of VU6019278.

  2019cites this paper
• The Modulation of Pain by Metabotropic Glutamate Receptors 7 and 8 in the Dorsal Striatum

  2019cites this paper
• Impact of the metabotropic glutamate receptor7 (mGlu7) allosteric agonist, AMN082, on fear learning and memory and anxiety-like behavior.

  2019cites this paper
• Fragment Based Approaches for Allosteric Metabotropic Glutamate Receptor (mGluR) Modulators.

  2019cites this paper
• Targeting epigenetic machinery: Emerging novel allosteric inhibitors.

  2019cites this paper
• Metabotropic glutamate receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database

  2019cites this paper
• Insights into the Structural Aspects of the mGlu Receptor Orthosteric Binding Site.

  2019cites this paper
• Metabotropic Glutamate Receptors and Neurological/Psychiatric Disorders

  2019influential citation
• Negative Allosteric Modulators of mGlu7 Receptor as Putative Antipsychotic Drugs

  2018influential citation
• Metabotropic glutamate receptor subtype 7 in the dorsal striatum oppositely modulates pain in sham and neuropathic rats

  2018influential citation
• Metabotropic Glutamate Receptor 7: A New Therapeutic Target in Neurodevelopmental Disorders

  2018influential citation
• Structural Basis for ( S)-3,4-Dicarboxyphenylglycine (DCPG) As a Potent and Subtype Selective Agonist of the mGlu8 Receptor.

  2018cites this paper
• Metabotropic glutamate receptors as targets for novel anxiolytics

  2018cites this paper
• Discovery of VU6005649, a CNS Penetrant mGlu7/8 Receptor PAM Derived from a Series of Pyrazolo[1,5-a]pyrimidines.

  2017cites this paper
• Pharmacogenetics and Pharmacotherapy of Military Personnel Suffering from Post-traumatic Stress Disorder

  2017cites this paper
• Metabotropic Glutamate Receptors in Amygdala Functions

  2017cites this paper
• Genetic Reduction or Negative Modulation of mGlu7 Does Not Impact Anxiety and Fear Learning Phenotypes in a Mouse Model of MECP2 Duplication Syndrome.

  2017cites this paper
• Metabotropic Glutamate Receptors – Regulation of Acute and Chronic Stress-Related Behavior and Physiology

  2017influential citation
• Recent advances in the medicinal chemistry of group II and group III mGlu receptors.

  2017cites this paper
• Relief from detrimental consequences of chronic psychosocial stress in mice deficient for the metabotropic glutamate receptor subtype 7

  2017cites this paper
• mGlu7 potentiation rescues cognitive, social, and respiratory phenotypes in a mouse model of Rett syndrome

  2017cites this paper
• Neurobiological insights and novel therapeutic opportunities for CNS disorders from mGlu receptor allosteric and biased modulation

  2017cites this paper
• The drug candidate, ADX71441, is a novel, potent and selective positive allosteric modulator of the GABAB receptor with a potential for treatment of anxiety, pain and spasticity

  2017cites this paper
• VU6010608, a Novel mGlu7 NAM from a Series of N-(2-(1H-1,2,4-Triazol-1-yl)-5-(trifluoromethoxy)phenyl)benzamides.

  2017cites this paper
• Nociception modulation by supraspinal group III metabotropic glutamate receptors

  2017cites this paper
• The Role of mGlu Receptors in Hippocampal Plasticity Deficits in Neurological and Psychiatric Disorders: Implications for Allosteric Modulators as Novel Therapeutic Strategies

  2016influential citation
• Metabotropic Glutamate Receptors in Central Nervous System Diseases.

  2016cites this paper
• The Emerging Role of Metabotropic Glutamate Receptors in the Pathophysiology of Chronic Stress-Related Disorders

  2016cites this paper
• Metabotropic Glutamate Receptor 7: From Synaptic Function to Therapeutic Implications

  2016cites this paper
• Radiosynthesis and evaluation of 5-methyl-N-(4-[(11)C]methylpyrimidin-2-yl)-4-(1H-pyrazol-4-yl)thiazol-2-amine ([(11)C]ADX88178) as a novel radioligand for imaging of metabotropic glutamate receptor subtype 4 (mGluR4).

  2016cites this paper
• Phasic and Tonic mGlu7 Receptor Activity Modulates the Thalamocortical Network

  2016cites this paper
• Practical Strategies and Concepts in GPCR Allosteric Modulator Discovery: Recent Advances with Metabotropic Glutamate Receptors.

  2016cites this paper
• Molecular Insights into Metabotropic Glutamate Receptor Allosteric Modulation s

  2015cites this paper
• Targeting type-2 metabotropic glutamate receptors to protect vulnerable hippocampal neurons against ischemic damage

  2015cites this paper
• GABAB receptors as a therapeutic strategy in substance use disorders: focus on positive allosteric modulators.

  2015cites this paper
• Negative allosteric modulation of the mGlu7 receptor reduces visceral hypersensitivity in a stress-sensitive rat strain

  2015influential citation
• Metabotropic Glutamate Receptor 7 (mGluR7) as a Target for the Treatment of Psychostimulant Dependence.

  2015influential citation
• Therapeutic potential of group III metabotropic glutamate receptor ligands in pain.

  2015cites this paper
• MMPIP, an mGluR7-selective negative allosteric modulator, alleviates pain and normalizes affective and cognitive behavior in neuropathic mice

  2015cites this paper
• Selective Negative Allosteric Modulation Of Metabotropic Glutamate Receptors – A Structural Perspective of Ligands and Mutants

  2015cites this paper
• Activation of Metabotropic Glutamate Receptor 7 Is Required for Induction of Long-Term Potentiation at SC-CA1 Synapses in the Hippocampus

  2015influential citation
• ActivationofMetabotropicGlutamateReceptor7Is RequiredforInductionofLong-TermPotentiationatSC- CA1SynapsesintheHippocampus

  2015cites this paper
• Molecular Insights into Metabotropic Glutamate Receptor Allosteric Modulation

  2015cites this paper
• Selective regulation of recombinantly expressed mGlu7 metabotropic glutamate receptors by G protein-coupled receptor kinases and arrestins.

  2014cites this paper
• Characterization of the Novel Positive Allosteric Modulator of the Metabotropic Glutamate Receptor 4 ADX88178 in Rodent Models of Neuropsychiatric Disorders

  2014cites this paper
• Identification of Positive Allosteric Modulators VU0155094 (ML397) and VU0422288 (ML396) Reveals New Insights into the Biology of Metabotropic Glutamate Receptor 7

  2014cites this paper
• Group III Metabotropic Glutamate Receptors: Pharmacology, Physiology and Therapeutic Potential

  2014cites this paper
• Progress toward advanced understanding of metabotropic glutamate receptors: structure, signaling and therapeutic indications.

  2014cites this paper
• Development of allosteric modulators of GPCRs for treatment of CNS disorders.

  2014cites this paper
• Opportunities and challenges in the discovery of allosteric modulators of GPCRs for treating CNS disorders

  2014cites this paper
• Investigating group III metabotropic glutamate receptors as novel therapeutic targets in Parkinson's disease and Levodopa-induced dyskinesia

  2014cites this paper
• Blocking Metabotropic Glutamate Receptor Subtype 7 (mGlu7) via the Venus Flytrap Domain (VFTD) Inhibits Amygdala Plasticity, Stress, and Anxiety-related Behavior♦

  2014influential citation
• Evaluation of peripheral versus central effects of GABAB receptor activation using a novel, positive allosteric modulator of the GABAB receptor ADX71943, a pharmacological tool compound with a fully peripheral activity profile

  2014cites this paper
• Nouveaux mécanismes d'action du récepteur mGlu7a dans le thalamus : de la synapse au comportement

  2014influential citation