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https://www.readbyqxmd.com/read/28088471/effects-of-group-i-metabotropic-glutamate-receptor-antagonists-on-sensitivity-to-reinforcer-magnitude-and-delayed-reinforcement-in-a-delay-discounting-task-in-rats-contribution-of-delay-presentation-order
#1
Justin R Yates, Katherine K Rogers, Benjamin T Gunkel, Nicholas A Prior, Mallory N Hughes, Sara M Sharpe, Hunter L Campbell, Anthony B Johnson, Margaret G Keller, Kerry A Breitenstein, Hansen N Shults
Metabotropic glutamate receptor 1 (mGluR1) blockade has been shown to decrease impulsive choice, as measured in delay discounting. However, several variables are known to influence an animal's discounting, including sensitivity to delayed reinforcement and sensitivity to reinforcer magnitude. The goal of this experiment was to determine the effects of mGluR1, as well as mGluR5, antagonism on these parameters. Forty Sprague Dawley rats were trained in delay discounting, in which consistently choosing a small, immediate reward reflects impulsive choice...
January 11, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28044255/mavoglurant-augmentation-in-ocd-patients-resistant-to-selective-serotonin-reuptake-inhibitors-a-proof-of-concept-randomized-placebo-controlled-phase-2-study
#2
Daniel Rutrick, Dan J Stein, Ganesan Subramanian, Brian Smith, Maurizio Fava, Gregor Hasler, Jang-Ho Cha, Fabrizio Gasparini, Toni Donchev, Magdalena Ocwieja, Donald Johns, Baltazar Gomez-Mancilla
INTRODUCTION: To determine if mavoglurant (modified release) as an augmentation therapy to selective serotonin reuptake inhibitors (SSRIs) could have beneficial effects reducing Yale-Brown Obsessive Compulsive Scale (Y-BOCS) total score in patients with obsessive-compulsive disorder (OCD) resistant to SSRI treatment. METHODS: This was a multicenter, randomized, double-blind, placebo-controlled, parallel-group, phase 2 study. Patients remained on their SSRI treatment and mavoglurant or placebo was added on...
January 2, 2017: Advances in Therapy
https://www.readbyqxmd.com/read/28030853/mglur5-cb1-and-neuroprotection
#3
EDITORIAL
Toniana G Carvalho, Juliana G Doria, Fabiola M Ribeiro
No abstract text is available yet for this article.
December 21, 2016: Oncotarget
https://www.readbyqxmd.com/read/28030475/spinal-intracellular-metabotropic-glutamate-receptor-5-mglur5-contributes-to-pain-and-c-fos-expression-in-a-rat-model-of-inflammatory-pain
#4
Kathleen Vincent, Shu Fan Wang, André Laferrière, Naresh Kumar, Terence J Coderre
Metabotropic glutamate receptor 5 (mGluR5) is an excitatory G-protein coupled receptor present in the spinal cord dorsal horn (SCDH) where it has a well-established role in pain. In addition to its traditional location on the cytoplasmic membrane, recent evidence shows that these receptors are present intracellularly on the nuclear membrane in the SCDH and are implicated in neuropathic pain. Nuclear mGluR5 is a functional receptor that binds glutamate entering the cell through the neuronal glutamate transporter (GT) EAAT3 and activates transcription factor c-fos, whereas plasma membrane mGluR5 is responsible for c-jun activation...
December 26, 2016: Pain
https://www.readbyqxmd.com/read/28028604/molecular-mechanisms-of-group-i-metabotropic-glutamate-receptor-mediated-ltp-and-ltd-in-basolateral-amygdala-in-vitro
#5
A Chen, W W Hu, X L Jiang, M Potegal, H Li
The roles of group I metabotropic glutamate receptors, metabotropic glutamate receptor 1 (mGluR1) and mGluR5, in regulating synaptic plasticity and metaplasticity in the basolateral amygdala (BLA) remain unclear. The present study examined mGluR1- and mGluR5-mediated synaptic plasticity in the BLA and their respective signaling mechanisms. Bath application of the group I mGluR agonist, 3,5-dihydroxyphenylglycine (DHPG) (20 μM), directly suppressed basal fEPSPs (84.5 ± 6.3% of the baseline). The suppressive effect persisted for at least 30 min after washout; it was abolished by the mGluR1 antagonist 7-(hydroxyimino)cyclopropa[b]chromen-1a-carboxylate ethyl ester (CPCCOEt) but was unaffected by the mGluR5 antagonist 2-methyl-6- (phenylethynyl)-pyridine (MPEP)...
December 28, 2016: Psychopharmacology
https://www.readbyqxmd.com/read/28019025/mtep-impedes-the-neuronal-polarization-and-the-activity-of-the-akt-nf-%C3%AE%C2%BAb-pathway-in-rat-hippocampal-neurons
#6
Xiaohua Zhang, Ming Hu, Lin Zhang, Jing An, Wenhui Yan, Zhichao Zhang, Jianxin Liu, Haixia Lu, Xinlin Chen, Yong Liu
Metabotropic glutamate receptor 5 (mGluR5) is extensively involved in neural survival, differentiation, dendritic morphology, synaptic plasticity, and neural circuit formation. However, little is known about its role in neuronal polarization and axon outgrowth. In this study, we applied the selective agonist (RS)-2-chloro-5-hydroxyphenylglycine sodium salt and antagonist 3-[(2-methyl-4-thaizolyl) ethynyl] pyridine (MTEP) of mGluR5 to the cultured hippocampal neurons to observe the neuronal polarization and axon outgrowth, and further explored the possible intracellular signal transduction pathway...
December 26, 2016: Journal of Neuroscience Research
https://www.readbyqxmd.com/read/28018172/app-causes-hyperexcitability-in-fragile-x-mice
#7
Cara J Westmark, Shih-Chieh Chuang, Seth A Hays, Mikolaj J Filon, Brian C Ray, Pamela R Westmark, Jay R Gibson, Kimberly M Huber, Robert K S Wong
Amyloid-beta protein precursor (APP) and metabolite levels are altered in fragile X syndrome (FXS) patients and in the mouse model of the disorder, Fmr1(KO) mice. Normalization of APP levels in Fmr1(KO) mice (Fmr1(KO) /APP(HET) mice) rescues many disease phenotypes. Thus, APP is a potential biomarker as well as therapeutic target for FXS. Hyperexcitability is a key phenotype of FXS. Herein, we determine the effects of APP levels on hyperexcitability in Fmr1(KO) brain slices. Fmr1(KO) /APP(HET) slices exhibit complete rescue of UP states in a neocortical hyperexcitability model and reduced duration of ictal discharges in a CA3 hippocampal model...
2016: Frontiers in Molecular Neuroscience
https://www.readbyqxmd.com/read/28008418/regulation-of-group-i-metabotropic-glutamate-receptors-by-mapk-erk-in-neurons
#8
Li-Min Mao, John Q Wang
Group I metabotropic glutamate receptors (mGluR1 and mGluR5 subtypes) are regulated by protein kinases. A recent focus is mitogen-activated protein kinases (MAPK). A prototypic subclass of MAPKs, extracellular signal-regulated kinases (ERK), is densely expressed in adult brain postmitotic neurons. This kinase resides in not only the cytoplasm around the nucleus, also the neuronal peripheral structures such as synapses. Recombinant ERK2 binds to C terminal tails of mGluR1a in vitro and native ERK1/2 forms complexes with mGluR1/5 in neurons in vivo...
2016: Journal of Nature and Science
https://www.readbyqxmd.com/read/27994742/development-of-1h-pyrazolo-3-4-b-pyridines-as-metabotropic-glutamate-receptor-5-positive-allosteric-modulators
#9
Matthew D Hill, Haiquan Fang, Jeffrey M Brown, Thaddeus Molski, Amy Easton, Xiaojun Han, Regina Miller, Melissa Hill-Drzewi, Lizbeth Gallagher, Michele Matchett, Michael Gulianello, Anand Balakrishnan, Robert L Bertekap, Kenneth S Santone, Valerie J Whiterock, Xiaoliang Zhuo, Joanne J Bronson, John E Macor, Andrew P Degnan
The metabotropic glutamate receptor 5 (mGluR5) is an attractive target for the treatment of schizophrenia due to its role in regulating glutamatergic signaling in association with the N-methyl-d-aspartate receptor (NMDAR). We describe the synthesis of 1H-pyrazolo[3,4-b]pyridines and their utility as mGluR5 positive allosteric modulators (PAMs) without inherent agonist activity. A facile and convergent synthetic route provided access to a structurally diverse set of analogues that contain neither the aryl-acetylene-aryl nor aryl-methyleneoxy-aryl elements, the predominant structural motifs described in the literature...
December 8, 2016: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27920147/accumbens-nnos-interneurons-regulate-cocaine-relapse
#10
Alexander C W Smith, Michael D Scofield, Jasper A Heinsbroek, Cassandra D Gipson, Daniela Neuhofer, Doug J Roberts-Wolfe, Sade Spencer, Neringa M Stankeviciute, Rachel Smith, Nicholas P Allen, Melissa R Lorang, William C Griffin, Heather A Boger, Peter W Kalivas
: Relapse to drug use can be initiated by drug-associated cues. The intensity of cue-induced relapse is correlated with the induction of transient synaptic potentiation (t-SP) at glutamatergic synapses on medium spiny neurons (MSNs) in the nucleus accumbens core (NAcore), and requires spillover of glutamate from prefrontal cortical afferents. We used a rodent self-administration/reinstatement model of relapse to show that cue-induced t-SP and reinstated cocaine-seeking result from glutamate spillover initiating a metabotropic glutamate receptor 5 (mGluR5)-dependent increase in nitric oxide (NO) production...
December 5, 2016: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/27886171/transduction-of-group-i-mglur-mediated-synaptic-plasticity-by-%C3%AE-arrestin2-signalling
#11
Andrew G Eng, Daniel A Kelver, Tristan P Hedrick, Geoffrey T Swanson
Conventional signalling by the group I metabotropic glutamate receptors, mGluR1 and mGluR5, occurs through G-protein coupling, but evidence suggests they might also utilize other, non-canonical effector pathways. Here we test whether group I mGluRs require β-arrestin signalling during specific forms of plasticity at hippocampal excitatory synapses. We find that genetic ablation of β-arrestin2, but not β-arrestin1, results in deficits in plasticity mediated by mGlu1 receptors in CA3 pyramidal neurons and by mGlu5 receptors in CA1 pyramidal neurons...
November 25, 2016: Nature Communications
https://www.readbyqxmd.com/read/27881780/negative-allosteric-modulation-of-mglur5-partially-corrects-pathophysiology-in-a-mouse-model-of-rett-syndrome
#12
Jifang Tao, Hao Wu, Amanda A Coronado, Elizabeth de Laittre, Emily K Osterweil, Yi Zhang, Mark F Bear
: Rett syndrome (RTT) is caused by mutations in the gene encoding methyl-CpG binding protein 2 (MECP2), an epigenetic regulator of mRNA transcription. Here, we report a test of the hypothesis of shared pathophysiology of RTT and fragile X, another monogenic cause of autism and intellectual disability. In fragile X, the loss of the mRNA translational repressor FMRP leads to exaggerated protein synthesis downstream of metabotropic glutamate receptor 5 (mGluR5). We found that mGluR5- and protein-synthesis-dependent synaptic plasticity were similarly altered in area CA1 of Mecp2 KO mice...
November 23, 2016: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/27878759/loss-of-adenylyl-cyclase-type-5-in-the-dorsal-striatum-produces-autistic-like-behaviors
#13
Hannah Kim, Yunjin Lee, Jin-Young Park, Ji-Eun Kim, Tae-Kyung Kim, Juli Choi, Jung-Eun Lee, Eun-Hwa Lee, Daesoo Kim, Kyoung-Shim Kim, Pyung-Lim Han
Autism spectrum disorders (ASDs) are a heterogeneous group of psychiatric illness characterized by common core symptoms including sociability deficits and stereotyped behaviors. ASD is caused by various genetic and non-genetic factors. The genetic effects of autism-related genes are usually global and are presented with multiple symptoms, which hamper understanding of the mechanism through which the diverse causes of ASD produce common symptoms. In the present study, we demonstrate that genetic or molecular disruption of an array of molecular networks centered on adenylyl cyclase type-5 (AC5 or ADCY5) in the dorsal striatum produces autistic-like behaviors...
November 23, 2016: Molecular Neurobiology
https://www.readbyqxmd.com/read/27872582/separate-ionotropic-and-metabotropic-glutamate-receptor-functions-in-depotentiation-vs-ltp-a-distinct-role-for-group1-mglur-subtypes-and-nmdars
#14
Amira Latif-Hernandez, Enrico Faldini, Tariq Ahmed, Detlef Balschun
Depotentiation (DP) is a mechanism by which synapses that have recently undergone long-term potentiation (LTP) can reverse their synaptic strengthening within a short time-window after LTP induction. Group 1 metabotropic glutamate receptors (mGluRs) were shown to be involved in different forms of LTP and long-term depression (LTD), but little is known about their roles in DP. Here, we generated DP by applying low-frequency stimulation (LFS) at 5 Hz after LTP had been induced by a single train of theta-burst-stimulation (TBS)...
2016: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/27856084/difluorocyclobutylacetylenes-as-positive-allosteric-modulators-of-mglur5-with-reduced-bioactivation-potential
#15
Andrew P Degnan, Darrell Maxwell, Anand Balakrishnan, Jeffrey M Brown, Amy Easton, Michael Gulianello, Umesh Hanumegowda, Melissa Hill-Drzewi, Regina Miller, Kenneth S Santone, Arun Senapati, Eric E Shields, Digavalli V Sivarao, Ryan Westphal, Valerie J Whiterock, Xiaoliang Zhuo, Joanne J Bronson, John E Macor
Schizophrenia is a serious illness that affects millions of patients and has been associated with N-methyl-d-aspartate receptor (NMDAR) hypofunction. It has been demonstrated that activation of metabotropic glutamate receptor 5 (mGluR5) enhances NMDA receptor function, suggesting the potential utility of mGluR5 positive allosteric modulators (PAMs) in the treatment of schizophrenia. Herein we describe the optimization of an mGluR5 PAM by replacement of a phenyl with aliphatic heterocycles and carbocycles as a strategy to reduce bioactivation in a biaryl acetylene chemotype...
December 15, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27847973/metabotropic-glutamate-receptor-5-as-a-potential-target-for-smoking-cessation
#16
REVIEW
Cristiano Chiamulera, Claudio Marcello Marzo, David J K Balfour
RATIONALE: Most habitual smokers find it difficult to quit smoking because they are dependent upon the nicotine present in tobacco smoke. Tobacco dependence is commonly treated pharmacologically using nicotine replacement therapy or drugs, such as varenicline, that target the nicotinic receptor. Relapse rates, however, remain high, and there remains a need to develop novel non-nicotinic pharmacotherapies for the dependence that are more effective than existing treatments. OBJECTIVE: The purpose of this paper is to review the evidence from preclinical and clinical studies that drugs that antagonise the metabotropic glutamate receptor 5 (mGluR5) in the brain are likely to be efficacious as treatments for tobacco dependence...
November 16, 2016: Psychopharmacology
https://www.readbyqxmd.com/read/27847228/metabotropic-glutamate-receptor-5-neuroimaging-in-schizophrenia
#17
Funda Akkus, Valerie Treyer, Simon M Ametamey, Anass Johayem, Alfred Buck, Gregor Hasler
The metabotropic glutamate receptor 5 (mGluR5) is a promising drug target for the treatment of schizophrenia. In this study, we compared mGluR5 distribution volume ration (DVR) in subjects with schizophrenia and healthy controls. Given our previous findings, we matched samples for gender, age, and smoking status. Binding to mGluR5 was determined using positron emission tomography and [(11)C]ABP688, which binds to an allosteric site with high selectivity. DVR in the 15 individuals with schizophrenia did not differ from that of the 15 controls...
November 12, 2016: Schizophrenia Research
https://www.readbyqxmd.com/read/27822496/estradiol-facilitation-of-cocaine-self-administration-in-female-rats-requires-activation-of-mglur5
#18
Luis A Martinez, Kellie S Gross, Brett T Himmler, Nicole L Emmitt, Brittni M Peterson, Natalie E Zlebnik, M Foster Olive, Marilyn E Carroll, Robert L Meisel, Paul G Mermelstein
In comparison to men, women initiate drug use at earlier ages and progress from initial use to addiction more rapidly. This heightened intake and vulnerability to drugs of abuse is regulated in part by estradiol, although the signaling mechanisms by which this occurs are not well understood. Recent findings indicate that within the nucleus accumbens core, estradiol induces structural plasticity via membrane-localized estrogen receptor α, functionally coupled to metabotropic glutamate receptor subtype 5 (mGluR5)...
September 2016: ENeuro
https://www.readbyqxmd.com/read/27796754/ketamine-self-administration-reduces-the-homeostasis-of-the-glutamate-synapse-in-the-rat-brain
#19
Lucia Caffino, Alessandro Piva, Giuseppe Giannotti, Marzia Di Chio, Francesca Mottarlini, Marco Venniro, David T Yew, Cristiano Chiamulera, Fabio Fumagalli
Ketamine is a non-competitive antagonist of the NMDA glutamate receptor with psychotomimetic and reinforcing properties, although recent work has pointed out its antidepressant action following acute exposure. Our aim was to investigate the expression of crucial components of the glutamate synapse following chronic ketamine self-administration (S/A), focusing our attention on medial prefrontal cortex (mPFC) and hippocampus (Hip), two brain regions involved in compulsive drug-seeking and drug-related cognitive disorders...
October 29, 2016: Molecular Neurobiology
https://www.readbyqxmd.com/read/27775719/astrocytes-mediate-neurovascular-signaling-to-capillary-pericytes-but-not-to-arterioles
#20
Anusha Mishra, James P Reynolds, Yang Chen, Alexander V Gourine, Dmitri A Rusakov, David Attwell
Active neurons increase their energy supply by dilating nearby arterioles and capillaries. This neurovascular coupling underlies blood oxygen level-dependent functional imaging signals, but its mechanism is controversial. Canonically, neurons release glutamate to activate metabotropic glutamate receptor 5 (mGluR5) on astrocytes, evoking Ca(2+) release from internal stores, activating phospholipase A2 and generating vasodilatory arachidonic acid derivatives. However, adult astrocytes lack mGluR5, and knockout of the inositol 1,4,5-trisphosphate receptors that release Ca(2+) from stores does not affect neurovascular coupling...
December 2016: Nature Neuroscience
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