Results 231 to 240 of about 12,245 (247)

Structure–Activity Relationships for Negative Allosteric mGluR5 Modulators

ChemMedChem, 2012
AbstractA series of compounds based on the mGluR5‐selective ligand 2‐methyl‐6‐(phenylethynyl)pyridine (MPEP) were designed and synthesized. The compounds were found to be either structural analogues of MPEP, substituted monomers, or dimeric analogues. All compounds retained mGluR5 selectivity with only weak or no activity at other mGluRs or iGluRs. The
Kaae, Birgitte H, Harpsøe, Kasper, Kvist, Trine, Mathiesen, Jesper M, Mølck, Christina, Gloriam, David E, Jimenez, Hermogenes N, Uberti, Michelle A, Nielsen, Søren M, Nielsen, Birgitte, Bräuner-Osborne, Hans, Sauerberg, Per, Clausen, Rasmus Prætorius, Madsen, Ulf   +13 more
openaire   +4 more sources

Azetidinyl oxadiazoles as potent mGluR5 positive allosteric modulators

Bioorganic & Medicinal Chemistry Letters, 2012
A novel series of aryl azetidinyl oxadiazoles are identified as mGluR5 positive allosteric modulators (PAMs) with improved physico-chemical properties. N-substituted cyclohexyl and exo-norbornyl carboxamides, and carbamate analogs of azetidines are moderate to potent mGluR5 PAMs.
Gamini Chandrasena, Xiaosui Pu, Christine G. Mazza Ferreira, Sang Phyo Hong, Mathivanan Packiarajan, Andrew D. White, Albert J. Robichaud, Robbin Brodbeck   +7 more
openaire   +3 more sources

Allosteric Modulation Mechanism of the mGluR5 Transmembrane Domain

Journal of Chemical Information and Modeling, 2019
Positive allosteric modulators (PAMs) of metabotropic glutamate receptor type 5 (mGluR5), a prototypical class C G protein-coupled receptor (GPCR), have shown therapeutic potential for various neurological disorders.
Xiaojing Cong, Jean-Baptiste Chéron, J. Golebiowski, S. Antonczak, S. Fiorucci   +4 more
semanticscholar   +1 more source

Imaging mGluR5 Dynamics in Astrocytes Using Quantum Dots

Current Protocols in Neuroscience, 2014
AbstractThis unit describes the method that we have developed to clarify endogenous mGluR5 (etabotropic tamate eceptors 5) dynamics in astrocytes by single‐particle tracking using quantum dots (QD‐SPT). QD‐SPT has been a powerful tool to examine the contribution of neurotransmitter receptor dynamics to synaptic plasticity.
Katsuhiko Mikoshiba, Misa Arizono, Hiroko Bannai   +2 more
openaire   +3 more sources

In vitro characterization of [3H]MethoxyPyEP, an mGluR5 selective radioligand

Life Sciences, 2003
We have characterized the in vitro properties of 3-[3H]methoxy-5-(pyridin-2-ylethynyl)pyridine ([3H]MethoxyPyEP), an analogue of the mGluR(5) receptor subtype antagonist MPEP [2-methyl-6-(phenylethynyl)-pyridine], in rat tissue preparations using tissue homogenates and autoradiography. Binding of [3H]MethoxyPyEP to rat cortex, hippocampus, thalamus and
Donald Burns, Terence G. Hamill, Stephen Krause, Ashok Chaudhary, Shil Patel, Raymond A. Gibson   +5 more
openaire   +3 more sources

Distribution of mGluR1α and mGluR5 immunolabeling in primate prefrontal cortex

Journal of Comparative Neurology, 2003
AbstractMetabotropic glutamate receptors (mGluRs) mediate important modulatory glutamatergic influences throughout the brain. However, the specific localization and functions of group I mGluR subtypes (mGluR1α and mGluR5) in cortical neurotransmission are not well known, particularly in primates. To address this issue, we used immunoelectron microscopy
Yoland Smith, Yoland Smith, E. Chris Muly, E. Chris Muly, Marcelia Maddox   +4 more
openaire   +3 more sources

A Role for mGluR5 Receptors in Intravenous Methamphetamine Self‐Administration

Annals of the New York Academy of Sciences, 2008
Selective antagonists of the mGluR5 receptor attenuate rewarding and reinforcing effects of various drugs of abuse, including alcohol, nicotine, and cocaine. However, the ability of mGluR5 antagonists to alter the reinforcing effects of methamphetamine has not yet been explored. In this study, male Sprague‐Dawley rats were trained to perform an operant
Megan P. H. Osborne, M. Foster Olive
openaire   +3 more sources

Structural and molecular determinants regulating mGluR5 surface expression

Neuropharmacology, 2017
Trafficking of G protein-coupled receptors (GPCRs) to the plasma membrane is a pivotal process to fulfill their biological functions. Metabotropic glutamate receptors (mGluRs; mGluR1-8) are expressed throughout the CNS and are important for modulating synaptic transmission and plasticity.
Kai Chang, Katherine W. Roche
openaire   +2 more sources

mGluR5-Mediated eCB Signaling in the Nucleus Accumbens Controls Vulnerability to Depressive-Like Behaviors and Pain After Chronic Social Defeat Stress

Molecular Neurobiology, 2021
Xiaotao Xu, Kaixuan Wu, Xiaqing Ma, Wenying Wang, Haiyan Wang, Min Huang, Limin Luo, Chen Su, Tifei Yuan, Haibo Shi, Ji Han, Aizhong Wang, Tao Xu   +12 more
semanticscholar   +1 more source

mGluR5 positive allosteric modulators

Drugs of the Future, 2008
P.J. Conn, Yelin Chen
openaire   +2 more sources