Results 201 to 210 of about 52,982 (243)

New 4-Functionalized Glutamate Analogues Are Selective Agonists at Metabotropic Glutamate Receptor Subtype 2 or Selective Agonists at Metabotropic Glutamate Receptor Group III

Journal of Medicinal Chemistry, 2016
The metabotropic glutamate (Glu) receptors (mGluRs) play key roles in modulating excitatory neurotransmission in the brain. In all, eight subtypes have been identified and divided into three groups, group I (mGlu1,5), group II (mGlu2,3), and group III (mGlu4,6-8).
Robb Brodbeck, Mette N. Erichsen, Amélie S. Tora, Amélie S. Tora, Thierry Gefflaut, Thierry Gefflaut, Emmanuelle Sagot, Emmanuelle Sagot, Cyril Goudet, Cyril Goudet, Christian Thomsen, Lennart Bunch, Birgitte Nielsen, Tri H. V. Huynh, Jean-Philippe Pin, Jean-Philippe Pin, Walden E. Bjørn-Yoshimoto, Zeinab Assaf, Zeinab Assaf, Tine B. Stensbøl   +19 more
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Metabotropic glutamate 2/3 receptors as drug targets

Current Opinion in Pharmacology, 2004
Metabotropic glutamate receptors are a family of class III G-protein-coupled receptors comprising eight members (mGluR1-8), which are an attractive target in the central nervous system because of the widespread use of glutamate as the principal excitatory amino acid transmitter.
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Biphenyl-indanones: Allosteric potentiators of the metabotropic glutamate subtype 2 receptor

Bioorganic & Medicinal Chemistry Letters, 2005
We have identified and synthesized a series of biphenyl-carboxylic acid indanones as allosteric potentiators of the metabotropic glutamate receptor 2. Structure-activity relationship studies directed toward improving the potency and the brain to plasma ratio of the initial lead led to the discovery of 5 and 23 (EC50=111 and 5 nM, respectively).
Celine Bonnefous, Theodore M. Kamenecka, Merryl Cramer, Hutchinson John H, Hervé Schaffhauser, Jean-Michel Vernier, Joyce K. James, Blake A. Rowe, Michael F. Gardner, Lorrie P. Daggett   +9 more
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A novel orally active Group 2 metabotropic glutamate receptor agonist

NeuroReport, 1997
Non-specific metabotropic glutamate receptor (mGluR) agonists have previously been shown to potentiate responses of spinal neurones to ionotropic glutamate receptor agonists. In this study we show that LY354740, which is a highly selective Group 2 mGluR agonist with nanomolar potency in vitro, also mimics the above effects following local ejection on ...
Ann Bond, James A. Monn, David M. Lodge
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Reduction of sensory and metabotropic glutamate receptor responses in the thalamus by the novel metabotropic glutamate receptor-1-selective antagonist S-2-methyl-4-carboxy-phenylglycine

Neuroscience, 1998
Previous work has shown that responses of thalamic neurons in vivo to the metabotropic glutamate receptor agonists 1S,3R-aminocyclopentane-1,3-dicarboxylate and S-3,5-dihydroxyphenylglycine can be reduced by a variety of phenylglycine antagonists. Responses of thalamic neurons to noxious thermal somatosensory stimuli were reduced in parallel by these ...
Salt, T. E., Turner, J. P.
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Role of group II metabotropic glutamate receptors 2/3 and group I metabotropic glutamate receptor 5 in developing rat medial vestibular nuclei

NeuroReport, 2005
In brainstem slices from developing rats, metabotropic glutamate receptors mGluR2/3 and mGluR5 play different inhibitory roles in synaptic transmission and plasticity of the medial vestibular nuclei. The mGluR2/3 block (LY341495) reduces the occurrence of long-term depression after vestibular afferent high frequency stimulation at P8-P10, and increases
GRASSI, Silvarosa, FRONDAROLI, Adele, PETTOROSSI, Vito Enrico   +2 more
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Metabotropic glutamate receptors 2 and 3 expressed by astrocytes in rat ventrobasal thalamus

Neuroscience Letters, 1999
It has been reported that pharmacologic activation of metabotropic receptors mGluR2/3 may produce inhibition of GABAergic transmission in rat ventrobasal thalamus. We use double immunolabeling to show that: (i) mGluR2/3 is expressed in glial processes surrounding GABAergic terminals, rather than in the terminals themselves, and (ii) mR2/3 positive ...
E Mineff, Juli G. Valtschanoff
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Localization of metabotropic glutamate receptors 2/3 on primary afferent axons in the rat

Neuroscience, 2001
The goal of the present study is to determine the relationship of metabotropic glutamate receptors 2/3 (mGluR2/3) to dorsal root ganglion cells, peripheral primary afferent fibers in digital nerves and central primary afferent fibers in the spinal cord.
Susan M. Carlton, Gregory L. Hargett, Richard E. Coggeshall   +2 more
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Metabotropic Glutamate 2 (mGlu2) Receptors and Schizophrenia Treatment

2017
Although it is not without controversy, recent preclinical and clinical studies suggest that activation of metabotropic glutamate 2 (mGlu2) receptors by orthosteric mGlu2/3 receptor agonists or allosteric mGlu2 receptor agonists represents a potential new approach to treat schizophrenia and other psychotic disorders.
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Pharmacological and molecular characterization of the positive allosteric modulators of metabotropic glutamate receptor 2

Neuropharmacology, 2016
The metabotropic glutamate receptor 2 (mGlu2) plays an important role in the presynaptic control of glutamate release and several mGlu2 positive allosteric modulators (PAMs) have been under assessment for their potential as antipsychotics. The binding mode of mGlu2 PAMs is better characterized in functional terms while few data are available on the ...
L, Lundström, C, Bissantz, J, Beck, M, Dellenbach, T J, Woltering, J, Wichmann, S, Gatti   +6 more
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