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https://www.readbyqxmd.com/read/28434782/dimeric-isoxazolyl-1-4-dihydropyridines-have-enhanced-binding-at-the-multi-drug-resistance-transporter
#1
Scott A Steiger, Chun Li, Donald S Backos, Philip Reigan, N R Natale
A series of dimeric isoxazolyl-1,4-dihydropyridines (IDHPs) were prepared by click chemistry and examined for their ability to bind the multi-drug resistance transporter (MDR-1), a member of the ATP-binding cassette superfamily (ABC). Eight compounds in the present study exhibited single digit micromolar binding to this efflux transporter. One monomeric IDHP m-Br-1c, possessed submicromolar binding of 510nM at MDR-1. Three of the dimeric IDHPs possessed <1.5µM activity, and 4b and 4c were observed to have superior binding selectivity compared to their corresponding monomers verses the voltage gated calcium channel (VGCC)...
April 8, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28433499/changes-in-the-expression-of-metabotropic-glutamate-receptor-5-mglur5-in-a-ketamine-based-animal-model-of-schizophrenia
#2
Dariusz Zurawek, Anna Salerno-Kochan, Marta Dziedzicka-Wasylewska, Agnieszka Nikiforuk, Tomasz Kos, Piotr Popik
It has been shown that the metabotropic glutamate receptor subtype 5 (mGluR5) is functionally associated with the NMDA subtype of the glutamate receptor family (NMDA receptors). These two receptors colocalize in brain regions associated with schizophrenia. Although the role of the NMDA receptor in cognitive and negative symptoms of schizophrenia is well studied, information about the role of mGluR5 receptors in schizophrenia is sparse. In our work, we show that subchronic administration of ketamine, a well-studied, non-competitive antagonist of NMDA receptors, caused cognitive deficits in rats as shown by testing novel object recognition (NOR)...
April 19, 2017: Schizophrenia Research
https://www.readbyqxmd.com/read/28405888/effects-of-common-grm5-genetic-variants-on-cognition-hippocampal-volume-and-mglur5-protein-levels-in-schizophrenia
#3
Natalie Matosin, Kelly Anne Newell, Yann Quidé, Jessica Lee Andrews, Nina Teroganova, Melissa Jayne Green, Francesca Fernandez
GRM5 (coding for metabotropic glutamate receptor 5, mGluR5) is a promising target for the treatment of cognitive deficits in schizophrenia, but there has been little investigation of its association with cognitive and brain phenotypes within this disorder. We examined the effects of common genetic variation in GRM5 with cognitive function, hippocampal volume, and hippocampal mGluR5 protein levels in schizophrenia patients relative to healthy controls. Two independent GRM5 variants rs60954128 [C>T] and rs3824927 [G>T] were genotyped in a schizophrenia case/control cohort (n=249/261)...
April 13, 2017: Brain Imaging and Behavior
https://www.readbyqxmd.com/read/28404748/components-of-rna-granules-affect-their-localization-and-dynamics-in-neuronal-dendrites
#4
Kazuhiko Mitsumori, Yosuke Takei, Nobutaka Hirokawa
In neurons, RNA transport is important for local protein synthesis. Messenger RNAs (mRNAs) are transported along dendrites as large RNA granules. The localization and dynamics of Puralpha and Stau1, major components of RNA transport granules, were investigated in cultured hippocampal neurons. Puralpha-positive granules were localized in both the shafts and spines of dendrites. In contrast, Stau1-positive granules tended to be localized mainly in dendritic shafts. More than 90% of Puralpha-positive granules were positive for Stau1 in immature dendrites, while only half were positive in mature dendrites...
April 12, 2017: Molecular Biology of the Cell
https://www.readbyqxmd.com/read/28397841/ketamine-induced-reduction-in-mglur5-availability-is-associated-with-an-antidepressant-response-an-11-c-abp688-and-pet-imaging-study-in-depression
#5
I Esterlis, N DellaGioia, R H Pietrzak, D Matuskey, N Nabulsi, C G Abdallah, J Yang, C Pittenger, G Sanacora, J H Krystal, R V Parsey, R E Carson, C DeLorenzo
The mechanisms of action of the rapid antidepressant effects of ketamine, an N-methyl-D-aspartate glutamate receptor antagonist, have not been fully elucidated. This study examined the effects of ketamine on ligand binding to a metabotropic glutamatergic receptor (mGluR5) in individuals with major depressive disorder (MDD) and healthy controls. Thirteen healthy and 13 MDD nonsmokers participated in two [(11)C]ABP688 positron emission tomography (PET) scans on the same day-before and during intravenous ketamine administration-and a third scan 1 day later...
April 11, 2017: Molecular Psychiatry
https://www.readbyqxmd.com/read/28395974/antidepressant-like-activity-of-icariin-mediated-by-group-i-mglurs-in-prenatally-stressed-offspring
#6
Xiaoxiao Zhang, Hongli Sun, Qian Su, Tianwei Lin, Huiping Zhang, Junli Zhang, Shaokang Dang, Zhongliang Zhu
OBJECTIVE: The present study was performed to identify antidepressant-like activity of icariin in prenatally stressed male rats. METHODS: The effects of icariin on PRS-induced depression were examined using sucrose preference test (SPT) and forced swimming test (FST) in male offspring, and measuring protein and mRNA expressions of group I mGluRs receptors and EAAT2 via western blotting and quantitative real-time PCR assays. RESULTS: The results indicated that prenatal restraint stress (PRS) resulted in several behavioral anomalies...
April 7, 2017: Brain & Development
https://www.readbyqxmd.com/read/28392767/early-onset-network-hyperexcitability-in-presymptomatic-alzheimer-s-disease-transgenic-mice-is-suppressed-by-passive-immunization-with-anti-human-app-a%C3%AE-antibody-and-by-mglur5-blockade
#7
Syed F Kazim, Shih-Chieh Chuang, Wangfa Zhao, Robert K S Wong, Riccardo Bianchi, Khalid Iqbal
Cortical and hippocampal network hyperexcitability appears to be an early event in Alzheimer's disease (AD) pathogenesis, and may contribute to memory impairment. It remains unclear if network hyperexcitability precedes memory impairment in mouse models of AD and what are the underlying cellular mechanisms. We thus evaluated seizure susceptibility and hippocampal network hyperexcitability at ~3 weeks of age [prior to amyloid beta (Aβ) plaque deposition, neurofibrillary pathology, and cognitive impairment] in a triple transgenic mouse model of familial AD (3xTg-AD mouse) that harbors mutated human Aβ precursor protein (APP), tau and presenilin 1 (PS1) genes...
2017: Frontiers in Aging Neuroscience
https://www.readbyqxmd.com/read/28392321/pharmacological-modulation-of-metabotropic-glutamate-receptor-subtype-5-and-7-impairs-extinction-of-social-fear-in-a-time-point-dependent-manner
#8
David A Slattery, Inga D Neumann, Peter J Flor, Iulia Zoicas
Pharmacological modulation of metabotropic glutamate receptor subtype 5 (mGluR5) and 7 (mGluR7) was shown to attenuate the acquisition and to facilitate the extinction of cued and contextual, non-social, fear. Using the allosteric mGluR5 antagonist 2-methyl-6-(phenylethynyl)-pyridine (MPEP) and the allosteric mGluR7 agonist N,N'-dibenzyhydryl-ethane-1,2-diamine dihydrochloride (AMN082), we aimed to study how pharmacological blockade of mGluR5 and activation of mGluR7 influence acquisition and extinction of social fear in mice...
April 7, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28365375/preclinical-molecular-imaging-of-glutamatergic-and-dopaminergic-neuroreceptor-kinetics-in-obsessive-compulsive-disorder
#9
S Servaes, D Glorie, J Verhaeghe, S Stroobants, S Staelens
BACKGROUND: Molecular neuroimaging was applied in the quinpirole rat model for compulsive checking in OCD to visualize the D2- and mGluR5-receptor occupancy with Raclopride and ABP-688 microPET/CT. METHODS: Animals (n=48) were exposed to either saline (CTRL; 1mL/kg) or quinpirole (QP; dopamine D2-agonist, 0.5mg/kg) in a single injection (RAC and ABP acute groups) or twice-weekly during 7weeks (chronic group). Animals underwent PET/CT after the 1st injection (acute) or before initial exposure and following the 10th injection in week 5 (chronic)...
March 30, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/28362857/a-novel-synaptic-junction-preparation-for-the-identification-and-characterization-of-cleft-proteins
#10
Amelia Burch, Jung-Hwa Tao-Cheng, Ayse Dosemeci
Identification of synaptic cleft components has been hampered by the lack of a suitable preparation enriched in synaptic junctions devoid of adjoining peripheral membranes. Prior strategies for the isolation of synaptic junctions, relying on detergents for the removal of peripheral membranes, resulted in substantial loss of membranes lining the cleft. Here, a novel, detergent-free method is described for the preparation of a synaptic junction (SJ) fraction, using phospholipase A2. Limited digestion of synaptic plasma membrane (SPM) fraction with phospholipase A2 followed by centrifugation over a sucrose cushion results in selective removal of membranes peripheral to the cleft while junctional membranes remain relatively intact as observed by electron microscopy...
2017: PloS One
https://www.readbyqxmd.com/read/28337838/the-selective-metabotropic-glutamate-receptor-5-antagonist-mavoglurant-afq056-reduces-the-incidence-of-reflux-episodes-in-dogs-and-patients-with-moderate-to-severe-gastroesophageal-reflux-disease
#11
M-L Rouzade-Dominguez, N Pezous, O J David, R Tutuian, S Bruley des Varannes, J Tack, P Malfertheiner, H-D Allescher, M Ufer, A Rühl
BACKGROUND: Transient lower esophageal sphincter relaxations (TLESRs) induced by gastric distension are modulated by the metabotropic glutamate receptor 5 (mGluR5) that influences the vagal reflex loop. We therefore aimed to examine the effects of the selective mGluR5 antagonist mavoglurant (AFQ056) on the number of TLESRs in dogs and reflux episodes in patients with gastroesophageal reflux disease (GERD). METHODS: In a dog model, the number of meal-induced TLESRs was determined after intravenous (0...
March 23, 2017: Neurogastroenterology and Motility: the Official Journal of the European Gastrointestinal Motility Society
https://www.readbyqxmd.com/read/28337539/homer1-vesl-1-in-the-rat-esophagus-focus-on-myenteric-plexus-and-neuromuscular-junction
#12
J Zimmermann, W L Neuhuber, M Raab
Homer1, a scaffolding protein of the postsynaptic density (PSD), enriched at excitatory synapses is known to anchor and modulate group I metabotropic glutamate receptors (mGluRs) and different channel- and receptor-proteins. Homer proteins are expressed in neurons of different brain regions, but also in non-neuronal tissues like skeletal muscle. Occurrence and location of Homer1 and mGluR5 in myenteric plexus and neuromuscular junctions (NMJ) of rat esophagus have yet not been characterized. We located Homer1 and mGluR5 immunoreactivity (-iry) in rat esophagus and focused on myenteric neurons, intraganglionic laminar endings (IGLEs) and NMJs, using double- and triple-label immunohistochemistry and confocal laser scanning microscopy...
March 23, 2017: Histochemistry and Cell Biology
https://www.readbyqxmd.com/read/28334166/grk5-regulates-social-behavior-via-suppression-of-mtorc1-signaling-in-medial-prefrontal-cortex
#13
Bing Niu, Peipei Liu, Minjie Shen, Cao Liu, Li Wang, Feifei Wang, Lan Ma
Impairments in social behaviors are features of a number of psychiatric diseases associated with subtle alterations in the medial prefrontal cortex (mPFC) circuitry. G protein-coupled receptor kinase (GRK) 5 is widely expressing in the cortex, however, its role in regulation of the mPFC activity and the development of social behaviors and psychiatric disorders is unclear. Here, we found that GRK5 dificiency in mice caused social behavior impairments. Further morphological, electrophysiological, and biochemical analyses showed abnormal postsynaptic ultrastructure, impaired excitatory synaptic transmission, the increased association of raptor with mTOR, and overactivated mTORC1-S6K signaling in the mPFC of Grk5-/- mice...
February 27, 2017: Cerebral Cortex
https://www.readbyqxmd.com/read/28306571/cns-syndromes-associated-with-antibodies-against-metabotropic-receptors
#14
Eric Lancaster
PURPOSE OF REVIEW: Autoantibodies to Central nervous system (CNS) metabotropic receptors are associated with a growing family of autoimmune brain diseases, including encephalitis, basal ganglia encephalitis, Ophelia syndrome, and cerebellitis. The purpose of this review is to summarize the state of knowledge regarding the target receptors, the neurological autoimmune disorders, and the pathogenic mechanisms. RECENT FINDINGS: Antibodies to the γ-aminobutyric acid B receptor are associate with limbic encephalitis and severe seizures, often with small cell lung cancers...
June 2017: Current Opinion in Neurology
https://www.readbyqxmd.com/read/28300633/the-medullary-dorsal-reticular-nucleus-as-a-relay-for-descending-pronociception-induced-by-the-mglur5-in-the-rat-infralimbic-cortex
#15
Ana David-Pereira, Boriss Sagalajev, Hong Wei, Armando Almeida, Antti Pertovaara, Filipa Pinto-Ribeiro
Metabotropic glutamate receptor 5 (mGluR5) activation in the infralimbic cortex (IL) induces pronociceptive behavior in healthy and monoarthritic rats. Here we studied whether the medullary dorsal reticular nucleus (DRt) and the spinal TRPV1 are mediating the IL/mGluR5-induced spinal pronociception and whether the facilitation of pain behavior is correlated with changes in spinal dorsal horn neuron activity. For drug administrations, all animals had a cannula in the IL as well as a cannula in the DRt or an intrathecal catheter...
March 11, 2017: Neuroscience
https://www.readbyqxmd.com/read/28270751/understanding-the-role-of-gpcr-heteroreceptor-complexes-in-modulating-the-brain-networks-in-health-and-disease
#16
REVIEW
Dasiel O Borroto-Escuela, Jens Carlsson, Patricia Ambrogini, Manuel Narváez, Karolina Wydra, Alexander O Tarakanov, Xiang Li, Carmelo Millón, Luca Ferraro, Riccardo Cuppini, Sergio Tanganelli, Fang Liu, Malgorzata Filip, Zaida Diaz-Cabiale, Kjell Fuxe
The introduction of allosteric receptor-receptor interactions in G protein-coupled receptor (GPCR) heteroreceptor complexes of the central nervous system (CNS) gave a new dimension to brain integration and neuropsychopharmacology. The molecular basis of learning and memory was proposed to be based on the reorganization of the homo- and heteroreceptor complexes in the postjunctional membrane of synapses. Long-term memory may be created by the transformation of parts of the heteroreceptor complexes into unique transcription factors which can lead to the formation of specific adapter proteins...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/28266711/pkc-epsilon-dependent-calcium-oscillations-associated-with-metabotropic-glutamate-receptor-5-prevent-agonist-mediated-receptor-desensitization-in-astrocytes
#17
Maxime Vergouts, Pierre J Doyen, Michael Peeters, Remi Opsomer, Thomas Michiels, Emmanuel Hermans
A critical role has been assigned to protein kinase C (PKC)ε in the control of intracellular calcium oscillations triggered upon activation of type 5 metabotropic glutamate receptor (mGluR5) in cultured astrocytes. Nevertheless, the physiological significance of this particular signalling profile in the response of astrocytes to glutamate remains largely unknown. Considering that kinases are frequently involved in the regulation of G protein-coupled receptors, we have examined a putative link between the nature of the calcium signals and the response regulation upon repeated exposures of astrocytes to the agonist (S)-3,5-dihydroxyphenylglycine...
March 7, 2017: Journal of Neurochemistry
https://www.readbyqxmd.com/read/28243714/nicotine-withdrawal-induced-inattention-is-absent-in-alpha7-nachr-knockout-mice
#18
K K Higa, A Grim, M E Kamenski, J van Enkhuizen, X Zhou, K Li, J C Naviaux, L Wang, R K Naviaux, M A Geyer, A Markou, J W Young
RATIONALE: Smoking is the leading cause of preventable death in the USA, but quit attempts result in withdrawal-induced cognitive dysfunction and predicts relapse. Greater understanding of the neural mechanism(s) underlying these cognitive deficits is required to develop targeted treatments to aid quit attempts. OBJECTIVES: We examined nicotine withdrawal-induced inattention in mice lacking the α7 nicotinic acetylcholine receptor (nAChR) using the five-choice continuous performance test (5C-CPT)...
February 28, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28231291/osteosarcoma-cell-proliferation-and-survival-requires-mglur5-receptor-activity-and-is-blocked-by-riluzole
#19
Sally Liao, Yuleisy Ruiz, Hira Gulzar, Zarina Yelskaya, Lyes Ait Taouit, Murielle Houssou, Trisha Jaikaran, Yuriy Schvarts, Kristina Kozlitina, Upal Basu-Roy, Alka Mansukhani, Shahana S Mahajan
Osteosarcomas are malignant tumors of bone, most commonly seen in children and adolescents. Despite advances in modern medicine, the poor survival rate of metastatic osteosarcoma has not improved in two decades. In the present study we have investigated the effect of Riluzole on a human and mouse metastatic osteosarcoma cells. We show that LM7 cells secrete glutamate in the media and that mGluR5 receptors are required for the proliferation of LM7 cells. Riluzole, which is known to inhibit glutamate release, inhibits proliferation, induces apoptosis and prevents migration of LM7 cells...
2017: PloS One
https://www.readbyqxmd.com/read/28213190/n-acetylcysteine-for-treating-cocaine-addiction-a-systematic-review
#20
REVIEW
Marco Antonio Nocito Echevarria, Tassio Andrade Reis, Giulianno Ruffo Capatti, Victor Siciliano Soares, Dartiu Xavier da Silveira, Thiago Marques Fidalgo
The aim of this paper is to extensively review the current literature available on N-acetylcysteine (NAC) treatment for cocaine dependence (clinical and experimental studies). We screened all articles published before February 2016 reporting on the use of NAC as a pharmacological intervention for cocaine dependence or discussed its potential as a therapeutic approach for cocaine dependence. We described our results qualitatively. 21 studies matched our search criteria: 6 clinical trials and 15 animal studies...
May 2017: Psychiatry Research
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