Results 241 to 250 of about 79,817 (291)

Chemical switch of a metabotropic glutamate receptor 2 silent allosteric modulator into dual metabotropic glutamate receptor 2/3 negative/positive allosteric modulators.

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.
S. Schann, Stanislas Mayer, C. Franchet, Mélanie Frauli, Edith Steinberg, M. Thomas, L. Baron, P. Neuville   +7 more
semanticscholar   +3 more sources

Progress in the developement of positive allosteric modulators of the metabotropic glutamate receptor 2.

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.
A. Trabanco, J. Cid, H. Lavreysen, G. Macdonald, G. Tresadern   +4 more
semanticscholar   +3 more sources

Aberrant expression of metabotropic glutamate receptor 2 in the vulnerable neurons of Alzheimer’s disease

Acta Neuropathologica, 2004
Selective neuronal dysfunction and degeneration are defining features of Alzheimer's disease (AD). While the exact mechanism(s) contributing to this selective neuronal vulnerability remains to be elucidated, we hypothesized that the differential expression of metabotropic glutamate receptors (mGluRs) may play a key role in this process since the ...
Hyoung-Gon Lee, Osamu Ogawa, Xiongwei Zhu, M. O'Neill, R. Petersen, R. Castellani, H. Ghanbari, George Perry, Mark A. Smith   +8 more
semanticscholar   +3 more sources

Metabotropic glutamate receptor 2/3 immunoreactivity in the developing rat cerebellar cortex

The Journal of Comparative Neurology, 1999
In 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 ...
Reiko Meguro, H. Ohishi, K. Hoshino, T. Hicks, M. Norita   +4 more
semanticscholar   +4 more sources

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.
M. Rudd, J. Mccauley
semanticscholar   +3 more sources

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
openaire   +2 more sources

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
openaire   +2 more sources

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.
openaire   +2 more sources

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
openaire   +3 more sources

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
openaire   +2 more sources