Expression and functional characterization of Metabotropic Glutamate Receptor Type 6 (mGluR6) in detergent micelles [PDF]
Biophysical Journal, 2009 Metabotropic glutamate receptors (mGluRs) are G protein coupled receptors which are implicated in different brain functions and dysfunctions including learning, memory, pain perception, neurodegeneration, schizophrenia and addiction. Metabotropic glutamate receptor type 6 (mGluR6) is a subtype of mGluRs which is exclusively expressed in ON-bipolar ...
Kalyan Tirupula +3 more
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Chronic interleukin‐6 exposure alters metabotropic glutamate receptor‐activated calcium signalling in cerebellar Purkinje neurons [PDF]
European Journal of Neuroscience, 2004 AbstractChronic central nervous system expression of the cytokine interleukin‐6 (IL‐6) is thought to contribute to the histopathological, pathophysiological, and cognitive deficits associated with various neurological disorders. However, the effects of chronic IL‐6 expression on neuronal function are largely unknown.
Thomas E. Nelson +2 more
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Protective effect of metabotropic glutamate mGluR5 receptor elimination in a 6-hydroxydopamine model of Parkinson's disease [PDF]
Neuroscience Letters, 2010 Pharmacologic or genetic blockade of metabotropic glutamate mGlu5 receptors (mGluR5) has been shown to attenuate parkinsonian motor deficits and protect nigrostriatal neurons from damage in the acute MPTP model of Parkinson's disease (PD), suggesting that therapeutically targeting the mGluR5 receptor may offer a novel approach to improving motor ...
Yolanda D. Black +5 more
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Discovery of 6-(pyrimidin-5-ylmethyl)quinoline-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5 [PDF]
Bioorganic & Medicinal Chemistry Letters, 2018 Based on previous work that established fused heterocycles as viable alternatives for the picolinamide core of our lead series of mGlu5 negative allosteric modulators (NAMs), we designed a novel series of 6-(pyrimidin-5-ylmethyl)quinoline-8-carboxamide mGlu5 NAMs.
Andrew S. Felts +9 more
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Immunohistological Studies of Metabotropic Glutamate Receptor Subtype 6-Deficient Mice Show No Abnormality of Retinal Cell Organization and Ganglion Cell Maturation [PDF]
The Journal of Neuroscience, 1999 Immature retinal ganglion cells (RGCs) initially show a multistratified dendritic pattern, and, during the postnatal period, these dendrites gradually monostratify into ON and OFF sublaminae. The selective agonist of group III metabotropic glutamate receptors (mGluR),l-2-amino-4-phosphonobutyrate (l-AP-4), hyperpolarizes ON bipolar cells and reduces ...
Yoshiaki Tagawa +4 more
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Metabotropic Glutamate Receptor 5 Upregulation in A-Fibers after Spinal Nerve Injury: 2-Methyl-6-(Phenylethynyl)-Pyridine (MPEP) Reverses the Induced Thermal Hyperalgesia [PDF]
The Journal of Neuroscience, 2002 Metabotropic glutamate receptor 5 (mGluR5) protein increased after sciatic nerve section in ipsilateral L4 and L5 DRG neuronal profiles, with most of the increase occurring in myelinated A-fiber somata. mGluR5 also increased in lamina II of the ipsilateral spinal cord and the proximal sciatic nerve stump in this model.
Lindsey Hudson +6 more
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2-Methyl-6-(phenylethynyl)pyridine Hydrochloride Modulates Metabotropic Glutamate 5 Receptors Endogenously Expressed in Zebrafish Brain [PDF]
ACS Chemical Neuroscience, 2016 Due to phylogenetic proximity to the human, zebrafish has been recognized as a reliable model to study Alzheimer's disease (AD) and other central nervous system disorders. Furthermore, metabotropic glutamate receptors have been previously reported to be impaired in brain from AD patients. Metabotropic glutamate 5 (mGlu5) receptors are G-protein coupled
José Luís Albasanz +5 more
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Frontiers in Neuroscience, 2021 Obesity is a multifactorial disease, which in turn contributes to the onset of comorbidities, such as diabetes and atherosclerosis. Moreover, there are only few options available for treating obesity, and most current pharmacotherapy causes severe ...
Tadeu P. D. Oliveira +12 more
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The Metabotropic Glutamate Receptor Subtype 5 Antagonist Fenobam Is Analgesic and Has Improved in Vivo Selectivity Compared with the Prototypical Antagonist 2-Methyl-6-(phenylethynyl)-pyridine [PDF]
The Journal of Pharmacology and Experimental Therapeutics, 2009 Metabotropic glutamate receptor subtype 5 (mGlu5) has been demonstrated to play a role in the modulation of numerous nociceptive modalities. When administered via peripheral, intrathecal, or systemic routes, mGlu5 antagonists have analgesic properties in a variety of preclinical pain models.
Michael C. Montana +5 more
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Frontiers in Molecular Neuroscience, 2022 Experimental studies on the pathogenetic process of paclitaxel-induced neuropathic pain (PINP) have been initially carried out, but PINP still has no effective therapy. Recently reported studies have highlighted the involvement of glutamate receptors and
Yize Li +10 more
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