Results 271 to 280 of about 593,014 (300)

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.
Christel Franchet, Pascal Neuville, Mélanie Frauli, Stanislas Mayer, Edith Steinberg, Luc Baron, Stephan Schann, Mireille Thomas   +7 more
openaire   +2 more sources

Activation of the extracellular signal‐regulated kinase 2 by metabotropic glutamate receptors

European Journal of Neuroscience, 1999
AbstractActivation 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., Baldani-Guerra B., Corsi M., Nakanishi S., Corti C.   +4 more
openaire   +3 more sources

Pyrimidine Methyl Anilines: Selective Potentiators for the Metabotropic Glutamate 2 Receptor

ChemInform, 2004
AbstractFor Abstract see ChemInform Abstract in Full Text.
Hu Essa H, Lida R. Tehrani, Jean-Michel Vernier, Peter C. Chua, Nicholas D. P. Cosford, Anthony B. Pinkerton, John H. Hutchinson, Blake A. Rowe, Johnny Y. Nagasawa   +8 more
openaire   +4 more sources

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.
Manuel Koller, Herman van der Putten, Shigetada Nakanishi, Will P.J.M Spooren, Rainer Kuhn, Fabrizio Gasparini   +5 more
openaire   +3 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).
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
openaire   +6 more sources

Positive allosteric modulators of the metabotropic glutamate receptor 2 for the treatment of schizophrenia

Expert Opinion on Therapeutic Patents, 2009
Normalization of excessive glutamate neurotransmission through activation of the metabotropic glutamate receptor 2 (mGluR2) represents a novel and promising approach for the treatment of schizophrenia. This strategy has gained support through the evaluation of dual mGluR2/3 agonists that act directly at the glutamate (orthosteric) binding site ...
openaire   +3 more sources

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.
openaire   +2 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, Rudolph J. Castellani, Xiongwei Zhu, Osamu Ogawa, Hossein A. Ghanbari, Robert B. Petersen, George Perry, Mark A. Smith, Michael J. O'Neill   +8 more
openaire   +3 more sources

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
openaire   +2 more sources

Systemic therapy for hormone receptor‐positive/human epidermal growth factor receptor 2‐negative early stage and metastatic breast cancer

Ca-A Cancer Journal for Clinicians, 2023
Laura A Huppert, Hope S Rugo
exaly