Triptolide up-regulates metabotropic glutamate receptor 5 to inhibit microglia activation in the lipopolysaccharide-induced model of Parkinson’s disease
Sign Up to like & getrecommendations! Published in 2018 at "Brain, Behavior, and Immunity"
DOI: 10.1016/j.bbi.2018.04.006
Abstract: Metabotropic glutamate receptor (mGlu)5 regulates microglia activation, which contributes to inflammation. However, the role of mGlu5 in neuroinflammation associated with Parkinson's disease (PD) remains unclear. Triptolide (T10) exerts potent immunosuppressive and anti-inflammatory effects and protects… read more here.
Keywords: mglu5; t10; microglia activation; induced model ... See more keywords
Evaluation of Synthetic Cytochrome P450-Mimetic Metalloporphyrins To Facilitate “Biomimetic” Biotransformation of a Series of mGlu5 Allosteric Ligands
Sign Up to like & getrecommendations! Published in 2019 at "ACS Omega"
DOI: 10.1021/acsomega.9b02017
Abstract: Allosteric ligands within a given chemotype can have the propensity to display a wide range of pharmacology, as well as unexpected changes in GPCR subtype selectivity, typically mediated by single-atom modifications to the ligand. Due… read more here.
Keywords: mglu5; allosteric ligands; synthetic cytochrome; pharmacology ... See more keywords
Altered Expression and in vivo Activity of mGlu5 variant a Receptors in the striatum of BTBR mice: Novel insights into the pathophysiology of adult idiopathic forms of autism spectrum disorders.
Sign Up to like & getrecommendations! Published in 2022 at "Current neuropharmacology"
DOI: 10.2174/1567202619999220209112609
Abstract: mGlu5 metabotropic glutamate receptors are considered as candidate drug targets in the treatment of "monogenic" forms of autism spectrum disorders (ASD), such as Fragile-X syndrome (FXS). However, despite promising preclinical data, clinical trials using mGlu5… read more here.
Keywords: idiopathic forms; expression; btbr mice; mglu5 ... See more keywords
Insights into the Metabolism, Disposition, and Quantitative Profile of mGlu5 NAM AE90015 with Metabolite Identification and a Novel Integration Method
Sign Up to like & getrecommendations! Published in 2024 at "Molecules"
DOI: 10.3390/molecules29235724
Abstract: AE90015 is a highly specific and effective negative allosteric modulator (NAM) for the human mGlu5 receptor, showing significant promise for treating Parkinson’s disease. An in vivo rat oral dose study was conducted on AE90015, which… read more here.
Keywords: method; mglu5; metabolism; disposition ... See more keywords
A ‘double-edged’ role for type-5 metabotropic glutamate receptors in pain disclosed by light-sensitive drugs
Sign Up to like & getrecommendations! Published in 2024 at "eLife"
DOI: 10.7554/elife.94931
Abstract: We used light-sensitive drugs to identify the brain region-specific role of mGlu5 metabotropic glutamate receptors in the control of pain. Optical activation of systemic JF-NP-26, a caged, normally inactive, negative allosteric modulator (NAM) of mGlu5… read more here.
Keywords: sensitive drugs; glutamate receptors; mglu5 receptor; light sensitive ... See more keywords