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mGlu2/3 receptor antagonists for depression: overview of underlying mechanisms and clinical development
Triggered by the ground-breaking finding that ketamine exerts robust and rapid-acting antidepressant effects in patients with treatment-resistant...
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Interaction of hallucinogenic rapid-acting antidepressants with mGlu2/3 receptor ligands as a window for more effective therapies
The desire to find a gold-standard therapy for depression is still ongoing. Develo** one universal and effective pharmacotherapy remains...
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mGlu2/3 Receptor Antagonists as Rapid-Acting Antidepressants
Since the discovery of the robust and rapid-acting antidepressant effects of ketamine in patients with treatment-resistant depression, the...
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Effects of the mGlu2/3 receptor agonist LY379268 on two models of disturbed auditory evoked brain oscillations in mice
Cognitive impairment is a core feature of schizophrenia and is poorly addressed by currently available medication. This is partly because the...
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Group I and group II metabotropic glutamate receptors are upregulated in the synapses of infant rats prenatally exposed to valproic acid
RationaleAutism spectrum disorder (ASD) is a neurodevelopmental disorder characterized by impaired social interaction and restricted/stereotyped...
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Ceftriaxone and mGlu2/3 interactions in the nucleus accumbens core affect the reinstatement of cocaine-seeking in male and female rats
RationaleThe beta-lactam antibiotic ceftriaxone reliably attenuates the reinstatement of cocaine seeking. While the restoration of nucleus accumbens...
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Stepwise activation of a metabotropic glutamate receptor
Metabotropic glutamate receptors belong to a family of G protein-coupled receptors that are obligate dimers and possess a large extracellular...
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G-protein activation by a metabotropic glutamate receptor
Family C G-protein-coupled receptors (GPCRs) operate as obligate dimers with extracellular domains that recognize small ligands, leading to G-protein...
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Glutamate, Glutamatergic Drugs and Schizophrenia
Over the past two decades, increasing evidence from preclinical and human studies supports a major role of glutamatergic dysfunction in the...
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Evaluation of the effects of the mGlu2/3 antagonist LY341495 on dyskinesia and psychosis-like behaviours in the MPTP-lesioned marmoset
BackgroundWe have previously demonstrated that the metabotropic glutamate 2 and 3 (mGlu 2/3 ) antagonist LY341495 reverses the anti-dyskinetic and...
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Partial mGlu5 receptor NAM, M-5MPEP, induces rapid and sustained antidepressant-like effects in the BDNF-dependent mechanism and enhances (R)-ketamine action in mice
BackgroundPartial negative allosteric modulators (NAM) of the metabotropic glutamate 5 (mGlu 5 ) receptor are an excellent alternative to full...
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Effects of Chronic Combined Treatment with Ketanserin and Fluoxetine in B6.CBA-D13Mit76C Recombinant Mice with Abnormal 5-HT1A Receptor Functional Activity
AbstractThe recombinant B6.CBA-D13Mit76C mouse strain is characterized by an altered sensitivity of 5-HT 1A receptors and upregulated 5-HT 1A gene...
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Effects of (S)-3,4-DCPG, an mGlu8 receptor agonist, on hippocampal long-term potentiation at perforant pathway-dentate gyrus synapses in prenatal valproic acid-induced rat model of autism
Autism spectrum disorder (ASD) is a pervasive neurodevelopmental condition characterized by social interaction deficits, communication impairments,...
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Biased signaling due to oligomerization of the G protein-coupled platelet-activating factor receptor
G protein-coupled receptors (GPCRs) are important drug targets that mediate various signaling pathways by activating G proteins and engaging...
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Optical Approaches for Modulating mGlu Receptor Activity
The metabotropic glutamate (mGlu) receptor family plays a diverse role in cellular function. However, differentiation of the specific contributions...
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Rapastinel alleviates the neurotoxic effect induced by NMDA receptor blockade in the early postnatal mouse brain
Rapastinel is a novel psychoactive substance that acts as an N-methyl-D-aspartate-receptor (NMDAR) agonist and triggers antidepressant- and...
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Modulation of DOM-Induced Head-Twitch Response by mGluR2 Agonist/Inverse Agonist is Associated with 5-HT2AR-Mediated Gs Signaling Pathway
Hallucinogenic 5-HT 2A receptor (5-HT 2A R) agonists-induced head-twitch response (HTR) is regulated by G s signaling pathway. Formation of heterodimers...
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Psychedelics action and schizophrenia
Psychedelics are compounds acting by serotonin 5-hydroxytryptamine (5-HT) 2A receptor activation and induce several behavioral responses. They are of...
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