Results 221 to 230 of about 48,931 (264)

Activation of metabotropic glutamate receptor 3 enhances interleukin (IL)-1β-stimulated release of IL-6 in cultured human astrocytes

Neuroscience, 2005
Previous studies have demonstrated that human astrocytes express mRNA and receptor protein for group I and II metabotropic glutamate receptors (mGluRs). Whether these receptors can influence the inflammatory and immune response and can modulate the capacity of astrocytes to produce inflammatory cytokines is still unclear.
Aronica, E., Gorter, J.A., Rozemuller, A.J.M., Yankaya, B., Troost, D.   +4 more
openaire   +6 more sources

Decreased metabotropic glutamate receptor type 1 availability in a patient with spinocerebellar ataxia type 6: A 11C-ITMM PET study

Journal of the Neurological Sciences, 2015
Imaging of metabotropic glutamate receptor type 1 (mGluR1), localized exclusively in the cerebellar Purkinje cells and related to cerebellar function, has recently become possible using positron emission tomography (PET). We report the initial mGluR1 imaging in a 74-year-old woman with spinocerebellar ataxia type 6 (SCA6).The patient and 9 age-matched ...
Yoshiharu Miura, Kenji Ishii, Kiichi Ishiwata, Kenji Ishibashi, Kinya Ishikawa   +4 more
openaire   +3 more sources

Mutational Analysis and Molecular Modeling of the Binding Pocket of the Metabotropic Glutamate 5 Receptor Negative Modulator 2-Methyl-6-(phenylethynyl)-pyridine

Molecular Pharmacology, 2003
Metabotropic glutamate (mGlu) 5 is a G-protein-coupled metabotropic glutamate receptor that plays an important role as a modulator of synaptic plasticity, ion channel activity, and excitotoxicity. 2-Methyl-6-(phenylethynyl)-pyridine (MPEP) is a highly potent, noncompetitive, selective, and systemically active antagonist of mGlu5 receptors.
Marie-Théeése Zenner, Christophe Fischer, Catherine Diener, Claudia Kratzeisen, Nicole A. Kratochwil, Jenny Piussi, Pari Malherbe, Porter Richard Hugh Phillip   +7 more
openaire   +3 more sources

Activation of spinal group I metabotropic glutamate receptors in rats evokes local glutamate release and spontaneous nociceptive behaviors: effects of 2-methyl-6-(phenylethynyl)-pyridine pretreatment

Neuroscience Letters, 2002
Intrathecal (i.t.) administration of the group I metabotropic glutamate receptor (mGluR) agonist (RS)-3,5-dihydroxyphenylglycine ((RS)-3,5-DHPG) to rats produces an immediate display of spontaneous nociceptive behaviors (SNBs) persisting for up to 10 h after injection (NeuroReport 7 (1996) 2743).
Jeffery J. Anderson, Lucia Correa, Daniel S. Lorrain, Mark A. Varney   +3 more
openaire   +3 more sources

Metabotropic glutamate receptor 5 antagonist 2-methyl-6-(phenylethynyl)pyridine produces antidepressant effects in rats: Role of brain-derived neurotrophic factor

Neuroscience, 2012
Recent studies highlight that the brain glutamate system is involved in the etiology of depression and glutamatergic-targeting drugs are currently being explored as novel antidepressant medications. Previous studies reveal that the selective metabotropic glutamate receptor 5 antagonist 2-methyl-6-(phenylethynyl)pyridine (MPEP) produces antidepressant ...
Yonghui Zhu, Danian Wei, X.X. Jiang, Chengyong Liu   +3 more
openaire   +3 more sources

Attenuation of Behavioral Effects of Cocaine by the Metabotropic Glutamate Receptor 5 Antagonist 2-Methyl-6-(phenylethynyl)-pyridine in Squirrel Monkeys: Comparison with Dizocilpine

The Journal of Pharmacology and Experimental Therapeutics, 2005
Growing evidence suggests a role for metabotropic glutamate receptors (mGluRs) in the behavioral effects of cocaine related to its abuse. The mGluR5 subtype, in particular, has come under scrutiny due to its distribution in brain regions associated with drug addiction.
Buyean Lee, James K. Rowlett, Roger D. Spealman, Adepero Shola Adewale, Donna M. Platt   +4 more
openaire   +3 more sources

Chronic, systemic treatment with a metabotropic glutamate receptor 5 antagonist in 6-hydroxydopamine partially lesioned rats reverses abnormal firing of dopaminergic neurons

Brain Research, 2009
Increasing evidence indicates that the excessive glutamate release onto substantia nigra pars compacta (SNpc) dopaminergic neurons may play an important role in the progression of nigral degeneration. We examined the effects of chronic, systemic treatment with 2-methyl-6-(phenylethynyl)-pyridine (MPEP), a selective metabotropic glutamate receptor 5 ...
Qiao Jun Zhang, Jian Liu, Jian Liu, Shuang Wang, Zhen Hua Gui, Umar Ali, Li Chen, Yong Wang   +7 more
openaire   +3 more sources

The metabotropic glutamate receptor antagonist 2‐methyl‐6‐(phenylethynyl) pyridine decreases striatal VGlut2 expression in association with an attenuation of L‐dopa‐induced dyskinesias

Synapse, 2011
AbstractThe striatal glutamatergic hyperactivity is considered critical in the development of levodopa‐induced dyskinesias (LID) in Parkinson's disease (PD). Pharmacological antagonism of the metabotropic glutamate receptors (mGluRs), in particular, the subtype mGluR5, can inhibit the expression of dyskinesia in both rodent and nonhuman primate models ...
Concepció Marin, Anna Jimenez, Mercè Bonastre, E. Aguilar   +3 more
openaire   +3 more sources

New positive allosteric modulators of the metabotropic glutamate receptor 2 (mGluR2): Identification and synthesis of N-propyl-8-chloro-6-substituted isoquinolones

Bioorganic & Medicinal Chemistry Letters, 2011
A series of N-propyl-8-chloro-6-substituted isoquinolones was identified as positive allosteric modulators of metabotropic glutamate receptor 2 (mGluR2 PAM) via high throughput screening (HTS). The subsequent synthesis and initial SAR exploration that led to the identification of compound 28 is described.
Jean-Philippe Rocher, Andrés A. Trabanco, Nadia Behaj, Yves Thollon, Guillaume Albert Jacques Duvey, Vanthea Nhem, Robert Johannes Lütjens, Philippe Cluzeau, Rocco Furnari, José María Cid, José Ignacio Andrés, Hassan Julien Imogai, Sonia Poli, Hilde Lavreysen, David D’Addona, Alexandre Raux, Gregor James Macdonald, Nicolas Poirier, Emmanuel Le Poul, Terry Patrick Finn, Géraldine Poulain   +20 more
openaire   +3 more sources

Pharmacological Effects of the Metabotropic Glutamate Receptor 1 Antagonist Compared with Those of the Metabotropic Glutamate Receptor 5 Antagonist and Metabotropic Glutamate Receptor 2/3 Agonist in Rodents: Detailed Investigations with a Selective Allosteric Metabotropic Glutamate Receptor 1 Antagonist, FTIDC [4-[1-(2-Fluoropyridine-3-yl)-5-methyl-1 H-1,2,3-triazol-4-yl]-N-isopropyl-N-methyl-3,6-dihydropyridine-1(2 H)-carboxamide]

The Journal of Pharmacology and Experimental Therapeutics, 2008
The functional roles of metabotropic glutamate receptor (mGluR) 1 in integrative brain functions were investigated using a potent and selective mGluR1 allosteric antagonist, FTIDC [4-[1-(2-fluoropyridine-3-yl)-5-methyl-1H-1,2,3-triazol-4-yl]-N-isopropyl-N-methyl-3,6-dihydropyridine-1(2H)-carboxamide], in comparison with the mGluR5 allosteric antagonist
Toshifumi Kimura, Miyuki Fukushima, Satoru Ito, Shunsuke Maehara, Hisashi Ohta, Satoko Ise, Hirohiko Hikichi, Gentaroh Suzuki, Hiroshi Kawamoto, Akio Satow, Takeshi Tanaka   +10 more
openaire   +2 more sources