Results 161 to 170 of about 49,403 (195)
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Metabotropic glutamate 2/3 receptors as drug targets
Current Opinion in Pharmacology, 2004Metabotropic 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, 2005We 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 +9 more
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Current Medicinal Chemistry, 2011
The metabotropic glutamate type 2 (mGlu2) receptor is a G-protein coupled receptor (GPCR) expressed on presynaptic nerve terminals where it negatively modulates glutamate and GABA release. Mixed mGlu2/mGlu3 orthosteric agonists such as LY354740 have shown activity in a range of preclinical animal models of anxiety and schizophrenia.
Hilde Lavreysen +4 more
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The metabotropic glutamate type 2 (mGlu2) receptor is a G-protein coupled receptor (GPCR) expressed on presynaptic nerve terminals where it negatively modulates glutamate and GABA release. Mixed mGlu2/mGlu3 orthosteric agonists such as LY354740 have shown activity in a range of preclinical animal models of anxiety and schizophrenia.
Hilde Lavreysen +4 more
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Positive Allosteric Modulators of the Metabotropic Glutamate Receptor Subtype 2 (mGluR2)
Current Topics in Medicinal Chemistry, 2005This article describes recent medicinal chemistry progress toward selective potentiators of the metabotropic glutamate receptor 2 (mGluR2). Groups at Lilly and Merck have identified new classes of potentiators that exhibit selectivity for mGluR2 over the seven other subtypes of mGluRs.
John A. McCauley, Michael T. Rudd
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Metabotropic glutamate receptor 2/3 immunoreactivity in the developing rat cerebellar cortex
The Journal of Comparative Neurology, 1999In adult rat cerebellar cortex, the metabotropic glutamate receptors (mGluRs) 2 and 3 (mGluR2/3) are present in somata, dendrites, and terminals of Golgi cells as well as in presumed glial processes (Ohishi et al. [1994], Neuron 13:55-66). In the present study, spatiotemporal changes in immunostaining for mGluR2/3 were examined in postnatal rat ...
Meguro, R. +4 more
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A novel orally active Group 2 metabotropic glutamate receptor agonist
NeuroReport, 1997Non-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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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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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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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 +2 more
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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 +2 more
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Localization of metabotropic glutamate receptors 2/3 on primary afferent axons in the rat
Neuroscience, 2001The 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 +2 more
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Metabotropic glutamate receptors 2 and 3 expressed by astrocytes in rat ventrobasal thalamus
Neuroscience Letters, 1999It 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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