|
Schizophrenia
|
0.400 |
Biomarker
|
disease |
BEFREE |
However, more recent studies failed to show clinical efficacy of mGlu2/3 receptor agonism in schizophrenia patients.
|
30038413 |
2019 |
|
Schizophrenia
|
0.400 |
Biomarker
|
disease |
BEFREE |
This Review highlights the advances made over the past few years in elucidating the structural and functional mechanisms underlying crosstalk between 5-HT<sub>2A</sub> and mGlu2 receptors in preclinical models of schizophrenia.
|
30807107 |
2019 |
|
Schizophrenia
|
0.400 |
Biomarker
|
disease |
BEFREE |
Hence, selective positive allosteric modulators (PAMs) of mGlu1 receptors hold promise for the treatment of positive symptoms of schizophrenia. mGlu5 receptors are widely expressed in the CNS and regulate the activity of cells that are involved in the pathophysiology of schizophrenia, such as cortical GABAergic interneurons and microglial cells. mGlu5 receptor PAMs are under development for the treatment of schizophrenia and cater the potential to act as disease modifiers by restraining neuroinflammation. mGlu2 receptors have attracted considerable interest because they negatively modulate 5-HT<sub>2A</sub> serotonin receptor signaling in the cerebral cortex.
|
30890967 |
2019 |
|
Schizophrenia
|
0.400 |
Biomarker
|
disease |
BEFREE |
The inbred Roman High- (RHA-I) and Low- (RLA-I) Avoidance rat strains are a congenital neurobehavioral model, with the RHA-I displaying schizophrenia-related behaviors and serotonin 2A (5-HT2A) and metabotropic glutamate 2 (mGlu2) receptor alterations in the prefrontal cortex (PFC).
|
31228641 |
2019 |
|
Schizophrenia
|
0.400 |
Biomarker
|
disease |
BEFREE |
Negative phase 2 schizophrenia clinical trials with JNJ-40411813 and AZD8529 seem to have tempered the high expectations of the scientific community on the utility of mGlu2 PAMs for the treatment of schizophrenia.
|
31242055 |
2019 |
|
Schizophrenia
|
0.400 |
AlteredExpression
|
disease |
BEFREE |
Our data suggests levels of GRM2 are not altered in two cortical regions from subjects with mood disorders or schizophrenia.
|
30326345 |
2019 |
|
Schizophrenia
|
0.400 |
Biomarker
|
disease |
BEFREE |
The serotonin 2A (5-HT<sub>2A</sub>) and metabotropic glutamate 2 (mGlu2) receptors regulate each other and are associated with schizophrenia.
|
28265857 |
2018 |
|
Schizophrenia
|
0.400 |
Biomarker
|
disease |
BEFREE |
In summary, these data suggest that a shift towards increased availability (and G-protein coupling) of cortical 5-HT2A vs. mGlu2 receptors may represent a common neurobiological mechanism underlying the emergence of psychosis and cognitive deficits observed in subjects with meth use disorder and schizophrenia.
|
30240581 |
2018 |
|
Schizophrenia
|
0.400 |
Biomarker
|
disease |
BEFREE |
Conducting a comprehensive phenotyping of CD2-KO mice, we found that they displayed novelty-induced hyperlocomotion (a rodent correlate of positive symptoms of schizophrenia), that was largely resistant against D1- and D2-dopamine-receptor antagonism, but responsive to the mGluR2/3-agonist LY379268.
|
30301879 |
2018 |
|
Schizophrenia
|
0.400 |
Biomarker
|
disease |
BEFREE |
Our findings show that PRS mice are valuable model for the study of epigenetic mechanisms involved in the pathogenesis of schizophrenia and support the hypothesis that pharmacological modulation of mGlu2/3 receptors could impact the early phase of schizophrenia and related neurodevelopmental disorders by regulating epigenetic processes that lie at the core of the disorders.
|
30564095 |
2018 |
|
Schizophrenia
|
0.400 |
Biomarker
|
disease |
BEFREE |
Our results provide a mechanism for mGluR2/3 agonists against NMDAR hypofunction, which may prove to be beneficial in the prophylactic treatment of SZ.
|
29793154 |
2018 |
|
Schizophrenia
|
0.400 |
Biomarker
|
disease |
BEFREE |
Serotonin 5-HT<sub>2A</sub> and metabotropic glutamate 2 (mGlu2) are neurotransmitter G protein-coupled receptors (GPCRs) involved in the signaling mechanisms underlying psychosis and schizophrenia treatment.
|
30209534 |
2018 |
|
Schizophrenia
|
0.400 |
Biomarker
|
disease |
BEFREE |
In this study, we tested whether an early treatment targeting mGluR2 would be effective in ameliorating cognitive impairments in the methylazoxymethanol acetate (MAM) model of SCZ.
|
28213064 |
2017 |
|
Schizophrenia
|
0.400 |
Biomarker
|
disease |
BEFREE |
AZD8529, an mGluR2 positive allosteric modulator (PAM), failed to separate from placebo in a phase II schizophrenia trial.
|
27995279 |
2017 |
|
Schizophrenia
|
0.400 |
Biomarker
|
disease |
BEFREE |
Allosteric signaling through an mGlu2 and 5-HT2A heteromeric receptor complex and its potential contribution to schizophrenia.
|
26758213 |
2016 |
|
Schizophrenia
|
0.400 |
PosttranslationalModification
|
disease |
BEFREE |
The methylation of GRM2 and GRM5 greatly decreased the risk of schizophrenia in comparison to the reference unmethylated pattern [OR=0.38, 95% CI; 0.144-1.035, p=0.05; OR=0.06, 95% CI; 0.007-0.54.10, p=0.01], respectively.
|
23149219 |
2013 |
|
Schizophrenia
|
0.400 |
Biomarker
|
disease |
BEFREE |
Pharmacogenetic analysis of the mGlu2/3 agonist LY2140023 monohydrate in the treatment of schizophrenia.
|
21173788 |
2012 |
|
Schizophrenia
|
0.400 |
Biomarker
|
disease |
BEFREE |
We did not detect an association between GRM2 or HTR2A and schizophrenia.
|
20211215 |
2010 |
|
Schizophrenia
|
0.400 |
Biomarker
|
disease |
BEFREE |
Recent biochemical, preclinical and clinical findings support group II metabotropic glutamate receptors (mGluR2 and mGluR3) as a new approach to treat schizophrenia.
|
19707855 |
2009 |
|
Schizophrenia
|
0.400 |
Biomarker
|
disease |
BEFREE |
However, a recent breakthrough indicates clinical efficacy of a drug stimulating the metabotropic glutamate receptor II, LY2140023, which has improved efficacy for negative and cognitive symptoms of schizophrenia.
|
18759551 |
2008 |
|
Schizophrenia
|
0.400 |
Biomarker
|
disease |
CTD_human |
Schizophrenia subjects showed significant decreases in mRNA levels of GAD(67), GAD(65), GAT-1, mGluR2, and neuronal nitric oxide synthase.
|
18923069 |
2008 |
|
Schizophrenia
|
0.400 |
Biomarker
|
disease |
BEFREE |
These regulatory changes indicate that the 2AR-mGluR2 complex may be involved in the altered cortical processes of schizophrenia, and this complex is therefore a promising new target for the treatment of psychosis.
|
18297054 |
2008 |
|
Schizophrenia
|
0.400 |
AlteredExpression
|
disease |
BEFREE |
The expression of mGluR2, 3 in DA cells provide a mechanism for glutamate to modulate dopamine release in the human brain and this species-specific difference may be critical to understanding rodent models in schizophrenia.
|
18853337 |
2008 |
|
Schizophrenia
|
0.400 |
AlteredExpression
|
disease |
LHGDN |
The expression of mGluR2, 3 in DA cells provide a mechanism for glutamate to modulate dopamine release in the human brain and this species-specific difference may be critical to understanding rodent models in schizophrenia.
|
18853337 |
2008 |
|
Schizophrenia
|
0.400 |
Biomarker
|
disease |
BEFREE |
Group II mGlus (mGlu2 and mGlu3) have attracted considerable interest since the development of potent specific agonists that exhibit atypical antipsychotic-like activity and reports of a genetic association between the mGlu3 gene and schizophrenia.
|
17531207 |
2007 |