Results 261 to 270 of about 20,152 (283)

Encephalitis associated with anti-mGluR5 antibodies

Practical Neurology
A 30-year-old woman had 5 days of visual hallucinations, nystagmus, memory impairment and mutism. On examination, she was disorientated with reduced attention span, gaze-evoked nystagmus, paratonia and abnormal frontal reflexes. Cerebrospinal fluid (CSF) showed 80 cells, protein 0.41 g/L and glucose 3.2 mmol/L (plasma glucose 5.0 mmol/L).
Denison Alves Pedrosa, João Henrique Fregadolli Ferreira, Rene Gleizer, Rafael Bernhart Carra, Rachel Marin de Carvalho, Verena Endmayr, Romana Hoftberger, Lívia Almeida Dutra   +7 more
openaire   +2 more sources

Synthesis and evaluation of 1,2,4-methyltriazines as mGluR5 antagonists

Organic & Biomolecular Chemistry, 2011
In previous studies we showed that 3-(substituted phenylethynyl)-5-methyl[1,2,4]triazine analogues of MPEP were potent antagonists of glutamate-mediated mobilization of internal calcium in an mGluR5 in vitro efficacy assay. In the present study we report the synthesis and evaluation of six 3-(substituted biphenylethynyl)-5-methyl[1,2,4]triazines (5a-f),
Hernán A. Navarro, Moses G. Gichinga, F. Ivy Carroll, Elizabeth Butala, Brian P. Gilmour, Jeremy P. Olson   +5 more
openaire   +3 more sources

Relevance of the metabotropic glutamate receptor (mGluR5) in the regulation of NREM-REM sleep cycle and homeostasis: Evidence from mGluR5 (−/−) mice

Behavioural Brain Research, 2015
Sleep is a homeostatically regulated behavior and sleep loss evokes a proportional increase in sleep time and delta slow wave activity. Glutamate and pharmacological modulation of the metabotropic glutamate receptors (mGluR) signaling have been implicated in the organization of vigilance states. Here, the role of the mGluR5 on homeostatic regulation of
L. Raeymaekers, Thomas Steckler, A. Ahnaou, W.H.I.M. Drinkenbrug   +3 more
openaire   +3 more sources

mGluR5–PLCβ4–PKCβ2/PKCγ pathways in hippocampal CA1 pyramidal neurons in pilocarpine model of status epilepticus in mGluR5+/+ mice

Epilepsy Research, 2008
While it is generally accepted that phospholipase C (PLC) and protein kinase C (PKC) are down-stream proteins involved in metabotropic glutamate receptor 5 (mGluR5)-related signal transduction, we still do not know which subtype of PLC or PKC is specifically regulated after mGluR5 activation.
Liu, J.X., Tang, Y.C., Liu, Y., Tang, F.R.   +3 more
openaire   +3 more sources

Reduced stress‐induced hyperthermia in mGluR5 knockout mice

European Journal of Neuroscience, 2002
AbstractIt hs been suggested that metabotropic glutamate receptor subtype 5 (mGluR5) play a role in the expression of anxiety, based on anxiolytic‐like effects of the selective mGluR5 antagonist MPEP (2‐methyl‐6‐(phenylethynyl)pyridine) in rodent models of anxiety, including stress‐induced hyperthermia (SIH).
Mark A. Varney, Jesse Brodkin, N. Warren, M. Bradbury, C. Busse, Linda J. Bristow   +5 more
openaire   +3 more sources

Inhibition of human hepatic CYP isoforms by mGluR5 antagonists

Life Sciences, 2004
Characterization of new chemical entities for their potential to produce drug-drug interactions is an important aspect of early drug discovery screening. In the present study, the potential for three metabotropic glutamate receptor antagonists to interact with recombinant human CYPs was investigated.
Mitchell D. Green, Christopher D. King, Xiaohui Jiang   +2 more
openaire   +3 more sources

Azetidinyl oxadiazoles as potent mGluR5 positive allosteric modulators

Bioorganic & Medicinal Chemistry Letters, 2012
A novel series of aryl azetidinyl oxadiazoles are identified as mGluR5 positive allosteric modulators (PAMs) with improved physico-chemical properties. N-substituted cyclohexyl and exo-norbornyl carboxamides, and carbamate analogs of azetidines are moderate to potent mGluR5 PAMs.
Gamini Chandrasena, Xiaosui Pu, Christine G. Mazza Ferreira, Sang Phyo Hong, Mathivanan Packiarajan, Andrew D. White, Albert J. Robichaud, Robbin Brodbeck   +7 more
openaire   +3 more sources

Allosteric Modulation Mechanism of the mGluR5 Transmembrane Domain

Journal of Chemical Information and Modeling, 2019
Positive allosteric modulators (PAMs) of metabotropic glutamate receptor type 5 (mGluR5), a prototypical class C G protein-coupled receptor (GPCR), have shown therapeutic potential for various neurological disorders.
Xiaojing Cong, Jean-Baptiste Chéron, J. Golebiowski, S. Antonczak, S. Fiorucci   +4 more
semanticscholar   +1 more source

Structure–Activity Relationships for Negative Allosteric mGluR5 Modulators

ChemMedChem, 2012
AbstractA series of compounds based on the mGluR5‐selective ligand 2‐methyl‐6‐(phenylethynyl)pyridine (MPEP) were designed and synthesized. The compounds were found to be either structural analogues of MPEP, substituted monomers, or dimeric analogues. All compounds retained mGluR5 selectivity with only weak or no activity at other mGluRs or iGluRs. The
Kaae, Birgitte H, Harpsøe, Kasper, Kvist, Trine, Mathiesen, Jesper M, Mølck, Christina, Gloriam, David E, Jimenez, Hermogenes N, Uberti, Michelle A, Nielsen, Søren M, Nielsen, Birgitte, Bräuner-Osborne, Hans, Sauerberg, Per, Clausen, Rasmus Prætorius, Madsen, Ulf   +13 more
openaire   +4 more sources

Imaging mGluR5 Dynamics in Astrocytes Using Quantum Dots

Current Protocols in Neuroscience, 2014
AbstractThis unit describes the method that we have developed to clarify endogenous mGluR5 (etabotropic tamate eceptors 5) dynamics in astrocytes by single‐particle tracking using quantum dots (QD‐SPT). QD‐SPT has been a powerful tool to examine the contribution of neurotransmitter receptor dynamics to synaptic plasticity.
Katsuhiko Mikoshiba, Misa Arizono, Hiroko Bannai   +2 more
openaire   +3 more sources