Results 21 to 30 of about 13,221 (154)

Natural Negative Allosteric Modulators of 5-HT3 Receptors [PDF]

Molecules, 2018
Chemotherapy-induced nausea and vomiting (CINV) remain the most common and devastating side-effects associated with cancer chemotherapy. In recent decades, several lines of research emphasize the importance of 5-hydroxytryptamine3 (5-HT3; serotonin) receptors in the pathogenesis and treatment of CINV.
Lina T. Al Kury, Mohamed Mahgoub, Frank Christopher Howarth, Murat Oz   +3 more
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Octahydropyrrolo[3,4-c]pyrrole negative allosteric modulators of mGlu1 [PDF]

Bioorganic & Medicinal Chemistry Letters, 2013
Development of SAR in an octahydropyrrolo[3,4-c]pyrrole series of negative allosteric modulators of mGlu1 using a functional cell-based assay is described in this Letter. The octahydropyrrolo[3,4-c]pyrrole scaffold was chosen as an isosteric replacement for the piperazine ring found in the initial hit compound. Characterization of selected compounds in
Jason T, Manka, Alice L, Rodriguez, Ryan D, Morrison, Daryl F, Venable, Hyekyung P, Cho, Anna L, Blobaum, J Scott, Daniels, Colleen M, Niswender, P Jeffrey, Conn, Craig W, Lindsley, Kyle A, Emmitte   +10 more
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Discovery of Novel Gq-Biased LPA1 Negative Allosteric Modulators [PDF]

SLAS Discovery, 2017
Lysophosphatidic acid (LPA) activates the G-protein-coupled receptor LPA1, which regulates various cellular processes, including cell proliferation and migration. Although LPA1 transduces cellular responses via Gq, Gi, and G12/13, associations between these signaling molecules and cellular phenotypes remain poorly characterized due to the lack of ...
Yuji, Shimizu, Masaharu, Nakayama
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Negative Allosteric Modulators of mGlu7 Receptor as Putative Antipsychotic Drugs [PDF]

Frontiers in Molecular Neuroscience, 2018
The data concerning antipsychotic-like activity of negative allosteric modulators (NAMs)/antagonists of mGlu7 receptors are limited. The only available ligands for this receptor are MMPIP and ADX71743. In the present studies, we used stable cell line expressing mGlu7 receptor and it was shown that both compounds dose-dependently potentiated forskolin ...
Cieslik, Paulina, Wozniak, Monika, Kaczorowska, K, Branski, Piotr, Burnat, Grzegorz, Chocyk, A, Bobula, B, Gruca, P, Litwa, E, Palucha-Poniewiera, A, Wasik, A, Pilc, A, Wieronska, Joanna   +12 more
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Allosterism vs. Orthosterism: Recent Findings and Future Perspectives on A2B AR Physio-Pathological Implications

Frontiers in Pharmacology, 2021
The development of GPCR (G-coupled protein receptor) allosteric modulators has attracted increasing interest in the last decades. The use of allosteric modulators in therapy offers several advantages with respect to orthosteric ones, as they can fine ...
Elisabetta Barresi, Claudia Martini, Federico Da Settimo, Giovanni Greco, Sabrina Taliani, Chiara Giacomelli, Maria Letizia Trincavelli   +6 more
doaj   +1 more source

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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Allosteric Modulation of Muscarinic Acetylcholine Receptors

Pharmaceuticals, 2010
An allosteric modulator is a ligand that binds to an allosteric site on the receptor and changes receptor conformation to produce increase (positive cooperativity) or decrease (negative cooperativity) in the binding or action of an orthosteric agonist (e.
Esam E. El-Fakahany, Jan Jakubík
doaj   +1 more source

Affecting AMPA Receptor Biophysical Gating Properties with Negative Allosteric Modulators

Molecular Neurobiology, 2022
Glutamatergic chemical synapses mediate excitatory neurotransmission by the ion flow through α-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA)-type glutamate receptors in the central nervous system (CNS). AMPA receptor-mediated synaptic transmission abnormalities may play a role in neurologic and neurodegenerative diseases, and compounds ...
Mohammad Qneibi, Mohammad Hawash, Nidal Jaradat, Sosana Bdir   +3 more
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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, P. Jeffrey Conn   +1 more
doaj   +1 more source

Modulation of the Erwinia ligand-gated ion channel (ELIC) and the 5-HT3 receptor via a common vestibule site

eLife, 2020
Pentameric ligand-gated ion channels (pLGICs) or Cys-loop receptors are involved in fast synaptic signaling in the nervous system. Allosteric modulators bind to sites that are remote from the neurotransmitter binding site, but modify coupling of ligand ...
Marijke Brams, Cedric Govaerts, Kumiko Kambara, Kerry L Price, Radovan Spurny, Anant Gharpure, Els Pardon, Genevieve L Evans, Daniel Bertrand, Sarah CR Lummis, Ryan E Hibbs, Jan Steyaert, Chris Ulens   +12 more
doaj   +1 more source