Results 241 to 250 of about 55,195 (280)

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).
Huynh, Tri H. V., Erichsen, Mette N., Tora, Amélie S., Goudet, Cyril, Sagot, Emmanuelle, Assaf, Zeinab, Thomsen, Christian, Brodbeck, Robb, Stensbøl, Tine B., Bjørn-Yoshimoto, Walden E., Nielsen, Birgitte, Pin, Jean-Philippe, Gefflaut, Thierry, Bunch, Lennart   +13 more
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Metabotropic Glutamate Receptor 2 Activators

2014
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 M. Cid, Andrés A. Trabanco, Hilde Lavreysen   +2 more
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Pyrimidine Methyl Anilines: Selective Potentiators for the Metabotropic Glutamate 2 Receptor

ChemInform, 2004
AbstractFor Abstract see ChemInform Abstract in Full Text.
Essa, Hu, Peter C, Chua, Lida, Tehrani, Johnny Y, Nagasawa, Anthony B, Pinkerton, Blake A, Rowe, Jean-Michel, Vernier, John H, Hutchinson, Nicholas D P, Cosford   +8 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 ...
A, Bond, J A, Monn, D, Lodge
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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).
Céline, Bonnefous, Jean-Michel, Vernier, John H, Hutchinson, Michael F, Gardner, Merryl, Cramer, Joyce K, James, Blake A, Rowe, Lorrie P, Daggett, Hervé, Schaffhauser, Theodore M, Kamenecka   +9 more
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LocaliZation of metabotropic glutamate receptor type 2 in the human brain

Neuroscience, 1999
Metabotropic 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 ...
T, Phillips, S, Rees, S, Augood, H, Waldvogel, R, Faull, C, Svendsen, P, Emson   +6 more
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Positive Allosteric Modulators of the Metabotropic Glutamate Receptor Subtype 2 (mGluR2)

Current Topics in Medicinal Chemistry, 2005
This 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.
Michael T, Rudd, John A, McCauley
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Lack of effect of LY314582 (a group 2 metabotropic glutamate receptor agonist) on phencyclidine-induced locomotor activity in metabotropic glutamate receptor 2 knockout mice

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.
W P, Spooren, F, Gasparini, H, van der Putten, M, Koller, S, Nakanishi, R, Kuhn   +5 more
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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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