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Cholesterol Localization around the Metabotropic Glutamate Receptor 2
The Journal of Physical Chemistry B, 2020The metabotropic glutamate receptor (mGluR) 2 plays a key role in the central nervous system. mGluR2 has been shown to be regulated by its surrounding lipid environment, especially by cholesterol, by an unknown mechanism. Here, using a combination of biochemical approaches, photo-cross-linking experiments, and molecular dynamics simulations we show the
Rainer D. Beck+9 more
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Pharmacology of Metabotropic Glutamate Receptor 2 Homo‐ and Heterodimers
The FASEB Journal, 2020Metabotropic Glutamate Receptors (mGluRs) are a family of class C g‐protein coupled receptors (GPCRs) that respond to glutamate as their native agonist. The eight members of the mGluR family are widely expressed across the nervous and are primarily charged with shaping and fine‐tuning neuronal excitability and synaptic efficacy. Like most class C GPCRs,
Paul J. Kammermeier+1 more
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Metabotropic Glutamate Receptor 2 Activators [PDF]
Schizophrenia is a common and severe, often disabling psychiatric illness of unknown aetiology that affects approximately 24 million people worldwide. The illness is characterized by symptomatology comprising positive symptoms (hallucinations and delusional behaviours), negative symptoms (anhedonia, social withdrawal and apathy) and cognitive ...
José María Cid+2 more
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LocaliZation of metabotropic glutamate receptor type 2 in the human brain
Neuroscience, 1999Metabotropic glutamate receptors are a heterogeneous family of G-protein-coupled receptors that are linked to multiple second messenger systems to regulate neuronal excitability and synaptic transmission. To elucidate the physiological role of these receptors in human central nervous system function and dysfunction at the receptor protein level ...
Sarah J. Augood+6 more
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Specificity of Metabotropic Glutamate Receptor 2 Coupling to G Proteins
Molecular Pharmacology, 2003Metabotropic glutamate receptor 2 (mGluR2) is a class 3 G protein-coupled receptor and an important mediator of synaptic activity in the central nervous system. Previous work demonstrated that mGluR2 couples to pertussis toxin (PTX)-sensitive G proteins. However, the specificity of mGluR2 coupling to individual members of the G(i/o) family is not known.
Paul J. Kammermeier+2 more
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Journal of Medicinal Chemistry, 2010
Using an mGluR2 FRET-based binding assay, binders of the transmembrane region devoid of functional activity were identified. It is reported that slight chemical modifications of these SAMs can dramatically change activity of the resulting analogues without altering their affinities.
Christel Franchet+7 more
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Using an mGluR2 FRET-based binding assay, binders of the transmembrane region devoid of functional activity were identified. It is reported that slight chemical modifications of these SAMs can dramatically change activity of the resulting analogues without altering their affinities.
Christel Franchet+7 more
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Activation of the extracellular signal‐regulated kinase 2 by metabotropic glutamate receptors
European Journal of Neuroscience, 1999AbstractActivation of metabotropic glutamate receptors (mGluRs) leads to modulation of a variety of second messenger pathways probably including the mitogen‐activated protein kinase (MAPK) extracellular signal‐regulated protein kinases (ERK). MAPK play a key role in the control of cellular responses to changes in the external environment by regulating ...
Ferraguti F.+4 more
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Pyrimidine Methyl Anilines: Selective Potentiators for the Metabotropic Glutamate 2 Receptor
ChemInform, 2004AbstractFor Abstract see ChemInform Abstract in Full Text.
Hu Essa H+8 more
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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+19 more
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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+19 more
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European Journal of Pharmacology, 2000
In metabotropic glutamate receptor 2 (mGlu(2)) knockout mice, the group 2 metabotropic glutamate receptor agonist LY314582 (20 mg/kg, i.p.), a racemate of LY354740, inhibits neither spontaneous nor phencyclidine (PCP)-induced (2.5 mg/kg, s.c.) locomotor activity.
Manuel Koller+5 more
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In metabotropic glutamate receptor 2 (mGlu(2)) knockout mice, the group 2 metabotropic glutamate receptor agonist LY314582 (20 mg/kg, i.p.), a racemate of LY354740, inhibits neither spontaneous nor phencyclidine (PCP)-induced (2.5 mg/kg, s.c.) locomotor activity.
Manuel Koller+5 more
openaire +3 more sources