Results 41 to 50 of about 121,181 (303)

Allosteric Modulators of G Protein-Coupled Dopamine and Serotonin Receptors: A New Class of Atypical Antipsychotics

Pharmaceuticals, 2020
Schizophrenia was first described by Emil Krapelin in the 19th century as one of the major mental illnesses causing disability worldwide. Since the introduction of chlorpromazine in 1952, strategies aimed at modifying the activity of dopamine receptors ...
Irene Fasciani, Francesco Petragnano, Gabriella Aloisi, Francesco Marampon, Marco Carli, Marco Scarselli, Roberto Maggio, Mario Rossi   +7 more
doaj   +1 more source

Affinity Mass Spectrometry-Based Fragment Screening Identified a New Negative Allosteric Modulator of the Adenosine A2A Receptor Targeting the Sodium Ion Pocket.

ACS Chemical Biology, 2021
Allosteric ligands provide new opportunities to modulate G protein-coupled receptor (GPCR) function and present therapeutic benefits over orthosteric molecules. Negative allosteric modulators (NAMs) can inhibit the activation of a receptor and downstream
Yan Lu, Hongyue Liu, Dehua Yang, Li Zhong, Ye Xin, Suwen Zhao, Ming-Wei Wang, Qingtong Zhou, W. Shui   +8 more
semanticscholar   +1 more source

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
openaire   +4 more sources

Discovery of a Negative Allosteric Modulator of GABA_B Receptors [PDF]

ACS Medicinal Chemistry Letters, 2014
Initialized from the scaffold of CGP7930, an allosteric agonist of GABAB receptors, a series of noncompetitive antagonists were discovered. Among these compounds, compounds 3, 6, and 14 decreased agonist GABA-induced maximal effect of IP3 production in HEK293 cells overexpressing GABAB receptors and Gqi9 proteins without changing the EC50. Compounds 3,
Lin-Hai, Chen, Bing, Sun, Yang, Zhang, Tong-Jie, Xu, Zhi-Xiong, Xia, Jian-Feng, Liu, Fa-Jun, Nan   +6 more
openaire   +2 more sources

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

Biochemical pharmacology of the positive allosteric modulation of the GABAb receptor "in Vitro" and "in Vivo" [PDF]

, 2007
Allosteric modulators of G-protein coupled receptors (GPCRs) interact with binding sites on the receptor molecule that are topographically distinct from the classic orthosteric site.
Gjoni, Tina
core   +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
openaire   +2 more sources

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
openaire   +2 more sources

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