Results 31 to 40 of about 5,023 (210)

Assessment of Quercetin Antiemetic Properties: In Vivo and In Silico Investigations on Receptor Binding Affinity and Synergistic Effects

Plants, 2023
Quercetin (QUA), a flavonoid compound, is ubiquitously found in plants and has demonstrated a diverse range of biological activities. The primary objective of the current study is to assess the potential antiemetic properties of QUA using an in vivo and ...
Raihan Chowdhury, Md. Shimul Bhuia, Asraful Islam Rakib, Rubel Hasan, Henrique Douglas Melo Coutinho, Isaac Moura Araújo, Irwin Rose Alencar de Menezes, Muhammad Torequl Islam   +7 more
doaj   +1 more source

Bitopic binding mode of an M1 muscarinic acetylcholine receptor agonist associated with adverse clinical trial outcomes [PDF]

, 2018
The realisation of the therapeutic potential of targeting the M1 muscarinic acetylcholine receptor (M1 mAChR) for the treatment of cognitive decline in Alzheimer's disease has prompted the discovery of M1 mAChR ligands showing efficacy in alleviating ...
Bradley, Sophie J., Broad, Lisa M., Brooke, Simon M., Bundgaard, Christoffer, Christopoulos, Arthur, Crabtree, Michael D., Dwomoh, Louis, Felder, Christian C., Langmead, Christopher J., Mogg, Adrian J., Molloy, Colin, Sanger, Helen E., Sexton, Patrick M., Thompson, Karen J., Tobin, Andrew B.   +14 more
core   +1 more source

Effects of novel muscarinic M3 receptor ligand C1213 in pulmonary arterial hypertension models. [PDF]

, 2016
Pulmonary hypertension (PH) is a complex disease comprising a pathologic remodeling and thickening of the pulmonary vessels causing an after load on the right heart ventricle that can result in ventricular failure. Triggered by oxidative stress, episodes
Ahmed, Mohamed, Al-Abed, Yousef, Coleman, Thomas, Lakshminrusimha, Satyanarayana, Patel, Hardik, VanPatten, Sonya   +5 more
core   +2 more sources

Virtual Affinity Fingerprints for Target Fishing: A New Application of Drug Profile Matching [PDF]

, 2013
We recently introduced Drug Profile Matching (DPM), a novel virtual affinity fingerprinting bioactivity prediction method. DPM is based on the docking profiles of ca.
Czobor, P., Hári, P., Jelinek, B., Málnási Csizmadia, András, Peragovics, Á., Simon, Z., Tombor, L.   +6 more
core   +1 more source

Distinct agonist regulation of muscarinic acetylcholine M2-M3 heteromers and their corresponding homomers [PDF]

, 2015
Each subtype of the muscarinic receptor family of G protein-coupled receptors is activated by similar concentrations of the neurotransmitter acetylcholine or closely related synthetic analogs such as carbachol. However, pharmacological selectivity can be
Alvarez-Curto, Elisa, Aslanoglou, Despoina, Marsango, Sara, Milligan, Graeme   +3 more
core   +1 more source

Mir-34a-5p Mediates Cross-Talk between M2 Muscarinic Receptors and Notch-1/EGFR Pathways in U87MG Glioblastoma Cells: Implication in Cell Proliferation [PDF]

, 2018
Glioblastoma (GBM) is the most aggressive human brain tumor. The high growth potential and decreased susceptibility to apoptosis of the glioma cells is mainly dependent on genetic amplifications or mutations of oncogenic or pro-apoptotic genes ...
Bevilacqua, Valeria, Caffarelli, Elisa, De Jaco, Antonella, Di Bari, Maria, Laneve, Pietro, Piovesana, Roberta, Talora, Claudio, Tata, Ada Maria, Trobiani, Laura   +8 more
core   +2 more sources

Identification of a Novel Allosteric Site at the M₅Muscarinic Acetylcholine Receptor

ACS Chemical Neuroscience, 2021
The M5 muscarinic acetylcholine receptor (mAChR) has emerged as an exciting therapeutic target for the treatment of addiction and behavioral disorders. This has been in part due to promising preclinical studies with the M5 mAChR selective negative allosteric modulator (NAM), ML375. The binding site of ML375 remains unknown, however, making it difficult
Wessel A. C. Burger, Patrick R. Gentry, Alice E. Berizzi, Ziva Vuckovic, Emma T. van der Westhuizen, Geoff Thompson, Mahmuda Yeasmin, Craig W. Lindsley, Patrick M. Sexton, Christopher J. Langmead, Andrew B. Tobin, Arthur Christopoulos, Celine Valant, David M. Thal   +13 more
openaire   +2 more sources

Assessment of the molecular mechanisms of action of novel 4-phenylpyridine-2-one and 6-phenylpyrimidin-4-one allosteric modulators at the M1 muscarinic acetylcholine receptors [PDF]

, 2018
Positive allosteric modulators (PAMs) that target the M1 muscarinic acetylcholine (ACh) receptor (M1 mAChR) are potential treatments for cognitive deficits in conditions such as Alzheimer's disease and schizophrenia.
Andrew B. Tobin, Arthur Christopoulos, Arthur Spathis, Ben Capuano, Celine Valant, Davoren, Ehlert, Ehlert, Elham Khajehali, Emma T. van der Westhuizen, Furchgott, Manuela Jörg, Mistry, Patrick M. Sexton, Peter J. Scammells, Shailesh N. Mistry   +15 more
core   +2 more sources

Multiple Residues in the Second Extracellular Loop Are Critical for M3 Muscarinic Acetylcholine Receptor Activation [PDF]

, 2007
Recent studies suggest that the second extracellular loop (o2 loop) of bovine rhodopsin and other class I G protein-coupled receptors (GPCRs) targeted by biogenic amine ligands folds deeply into the transmembrane receptor core where the binding of cis ...
Kim, Soo-Kyung, Li, Bo, Scarselli, Marco, Wess, Jürgen   +3 more
core   +1 more source

Interactions between the neuromodulatory systems and the amygdala: exploratory survey using the Allen Mouse Brain Atlas. [PDF]

, 2013
Neuromodulatory systems originate in nuclei localized in the subcortical region of the brain and control fundamental behaviors by interacting with many areas of the central nervous system.
Krichmar, Jeffrey L, Zaldivar, Andrew
core   +1 more source