ACS Medicinal Chemistry LettersThis Letter details our efforts to develop novel, non-acetylene-containing metabotropic glutamate receptor subtype 5 (mGlu5) negative allosteric modulators (NAMs) with improved pharmacological properties. This endeavor involved replacing the ether-linked pyrimidine moiety, a metabolic liability, with various 5-membered heterocycles. From this exercise,
Elizabeth S. Childress +20 more
openaire +3 more sources
Apo-state structure of the metabotropic glutamate receptor 5 transmembrane domain obtained using a photoswitchable ligand. [PDF]
Protein SciAbstract Metabotropic glutamate receptor 5 (mGlu5) is implicated in various neurodegenerative disorders, making it an attractive drug target. Although several ligand‐bound crystal structures of mGlu5 exist, their apo‐state crystal structure remains unknown.
Kondo Y +15 more
europepmc +2 more sources
Differential Epigenetic Regulation of Glutamatergic Synapse Pathway in Adults With Prenatal Exposure to Famine. [PDF]
Eur J NeurosciUsing DNA methylation data collected on adults prenatally exposed to the Chinese famine of 1959–1961, this study reports the altered epigenetic regulation in genes of the glutamate synapse pathway in association with early‐life adversity. Our analysis revealed an overall pattern of reduced DNA methylation of the pathway genes that is more pronounced in
Tan Z, Li W, Wang W, Zhang D, Tan Q.
europepmc +2 more sources
Topological analysis of small leucine-rich repeat proteoglycan nyctalopin. [PDF]
PLoS ONE, 2012 Nyctalopin is a small leucine rich repeat proteoglycan (SLRP) whose function is critical for normal vision. The absence of nyctalopin results in the complete form of congenital stationary night blindness.
Pasano Bojang, Ronald G Gregg
doaj +1 more source
First evidence for the presence of amino acid sensing mechanisms in the fish gastrointestinal tract
Scientific Reports, 2021 This study aimed to characterize amino acid sensing systems in the gastrointestinal tract (GIT) of the carnivorous fish model species rainbow trout. We observed that the trout GIT expresses mRNAs encoding some amino acid receptors described in mammals ...
Jessica Calo +5 more
doaj +1 more source
mGluR5 antagonism inhibits cocaine reinforcement and relapse by elevation of extracellular glutamate in the nucleus accumbens via a CB1 receptor mechanism. [PDF]
, 2018 Metabotropic glutamate receptor 5 (mGluR5) antagonism inhibits cocaine self-administration and reinstatement of drug-seeking behavior. However, the cellular and molecular mechanisms underlying this action are poorly understood.
Bi, Guo-Hua +9 more
core +2 more sources
G protein-coupled receptor signalling in astrocytes in health and disease: A focus on metabotropic glutamate receptors [PDF]
, 2012 Work published over the past 10–15 years has caused the neuroscience community to engage in a process of constant re-evaluation of the roles of glial cells in the mammalian central nervous system.
Bradley, Sophie J., Challiss, R.A. John
core +1 more source
Analgesia induced by the epigenetic drug, L-acetylcarnitine, outlasts the end of treatment in mouse models of chronic inflammatory and neuropathic pain [PDF]
, 2017 Background: L-acetylcarnitine, a drug marketed for the treatment of chronic pain, causes analgesia by epigenetically up-regulating type-2 metabotropic glutamate (mGlu2) receptors in the spinal cord.
Battaglia, Giuseppe +10 more
core +1 more source
Neuronal activity patterns in the mediodorsal thalamus and related cognitive circuits are modulated by metabotropic glutamate receptors. [PDF]
, 2015 The mediodorsal thalamus (MD) likely plays an important role in cognition as it receives abundant afferent connections from the amygdala and prefrontal cortex (PFC).
Copeland, CS, Neale, SA, Salt, TE
core +1 more source