Results 41 to 50 of about 107,657 (326)
Development of allosteric modulators of GPCRs for treatment of CNS disorders
Neurobiology of Disease, 2014 The discovery of allosteric modulators of G protein-coupled receptors (GPCRs) provides a promising new strategy with potential for developing novel treatments for a variety of central nervous system (CNS) disorders.
Hilary Highfield Nickols +1 more
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The unconventional activation of the muscarinic acetylcholine receptor M4R by diverse ligands
Nature Communications, 2022 The authors report the structural characterization of M4R selective allosteric agonist, compound-110, as well as agonist iperoxo and positive allosteric modulator LY2119620.
Jingjing Wang +15 more
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Positive Allosteric Modulators of Nicotinic Acetylcholine Receptor [PDF]
ACS Medicinal Chemistry Letters, 2013 Priority Application: Priority date: July 8, 2011 Inventors: Eskildsen, J.; Sams, A. G.; Pueschl, A. Assignee Company: H. Lundbeck A/S, Den. Disease Area: autism, neurodegenerative diseases Biological Target: nicotinic acetylcholine receptor α7 (α7 nAChR) Summary: The patent application claims cyclopropylcarboxamide derivatives as positive allosteric ...
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Nature Communications, 2021 Here, the authors use smFRET to assess the structural dynamics of metabotropic glutamate receptor mGlu2 and show that a positive allosteric modulator or the Gi protein stabilize mGlu2 in the glutamate-induced active state, leading to the full activation ...
Anne-Marinette Cao +5 more
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GABAA receptor: Positive and negative allosteric modulators [PDF]
Neuropharmacology, 2018 gamma-Aminobutyric acid (GABA)-mediated inhibitory neurotransmission and the gene products involved were discovered during the mid-twentieth century. Historically, myriad existing nervous system drugs act as positive and negative allosteric modulators of these proteins, making GABA a major component of modern neuropharmacology, and suggesting that many
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Contrasting properties of α7-selective orthosteric and allosteric agonists examined on native nicotinic acetylcholine receptors. [PDF]
PLoS ONE, 2013 Subtype-selective ligands are important tools for the pharmacological characterisation of neurotransmitter receptors. This is particularly the case for nicotinic acetylcholine receptors (nAChRs), given the heterogeneity of their subunit composition.
JasKiran K Gill +4 more
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LY404187: A Novel Positive Allosteric Modulator of AMPA Receptors [PDF]
CNS Drug Reviews, 2002 ABSTRACTLY404187 is a selective, potent and centrally active positive allosteric modulator of AMPA receptors. LY404187 preferentially acts at recombinant human homomeric GluR2 and GluR4 versus GluR1 and GluR3 AMPA receptors. In addition, LY404187 potentiates the flip splice variant of these AMPA receptors to a greater degree than the flop splice ...
Jennifer C, Quirk, Eric S, Nisenbaum
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The molecular mechanism of positive allosteric modulation at the dopamine D1 receptor
International Journal of Molecular Sciences, 2023 Abstract The dopamine D1 receptor (D1R) is a promising target for treating various psychiatric disorders. While upregulation of D1R activity has shown potential in alleviating motor and cognitive symptoms, orthosteric agonists have limitations, restricting their clinical applications. However, the discovery of several
Alexander Goldberg, Bing Xie, Lei Shi
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, 2020 The G protein-coupled receptor (GPCR) µ-opioid receptor (µOR) is one of several drug targets of commercially available therapeutics for pain. Various opioid drugs like morphines have been associated to numerous substance abuse-related deaths around the ...
Ricky, Nellas, Mac Kevin, Braza
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, 2023 International audienceThe α7 nicotinic acetylcholine receptor (nAChR), a potential drug target for treating cognitive disorders, mediates communication between neuronal and non- neuronal cells. Although many competitive antagonists, agonists, and partial-
Stéphanie Pons +21 more
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