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 +5 more
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Molecular Modeling of the M3 Acetylcholine Muscarinic Receptor and Its Binding Site [PDF]
Journal of Biomedicine and Biotechnology, 2012 The present study reports the results of a combined computational and site mutagenesis study designed to provide new insights into the orthosteric binding site of the human M3 muscarinic acetylcholine receptor. For this purpose a three-dimensional structure of the receptor at atomic resolution was built by homology modeling, using the crystallographic ...
Arnau Cordomí +4 more
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Is there a rationale and role for long-acting anticholinergic bronchodilators in asthma? [PDF]
, 2014 The authors acknowledge the medical writing assistance received from Sam Yarwood, PhD, of Complete HealthVizion, in the form of literature searches and preparation and revision of the draft manuscript.Peer reviewedPublisher ...
Fromer, Leonard +4 more
core +7 more sources
The Cholinergic Pathways in Inflammation: A Potential Pharmacotherapeutic Target for COPD
Frontiers in Pharmacology, 2018 In COPD, the activity of the cholinergic system is increased, which is one of the reasons for the airflow limitation caused by the contraction of airway smooth muscles.
Mitsuhiro Yamada, Masakazu Ichinose
doaj +1 more source
Structure-guided development of selective M3 muscarinic acetylcholine receptor antagonists [PDF]
Proceedings of the National Academy of Sciences, 2018 Significance The development of selective antagonists for muscarinic acetylcholine receptors is challenging due to high homology in orthosteric binding sites among subtypes. Starting from a single amino acid difference in the orthosteric pockets in M2 muscarinic acetylcholine receptor (M2R) and M3R, we developed an M3R-selective antagonist ...
Inbar Fish +20 more
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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. +14 more
core +1 more source
Allosteric interactions at the M3 muscarinic acetylcholine receptor
, 2023 The extracellular loops of muscarinic acetylcholine receptors are predicted to play a role in the binding and regulation of allosteric modulators. Furthermore, the sequence of the five subtypes of muscarinic receptors shows a large degree of diversity in this region.
openaire +4 more sources
Muscarinic receptor oligomerization [PDF]
, 2018 G protein-coupled receptors (GPCRs) have been classically described as monomeric entities that function by binding in a 1:1 stoichiometric ratio to both ligand and downstream signalling proteins.
Alvarez-Curto, Elisa +3 more
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Cholinergic receptor alterations in the cerebral cortex of spinal cord injured rat
Biochemistry and Biophysics Reports, 2017 Many areas of the cerebral cortex process sensory information or coordinate motor output necessary for control of movement. Disturbances in cortical cholinergic system can affect locomotor coordination.
R. Chinthu, T.R. Anju, C.S. Paulose
doaj +1 more source
M3 muscarinic acetylcholine receptor facilitates the endocytosis of mu opioid receptor mediated by morphine independently of the formation of heteromeric complexes [PDF]
, 2017 Morphine inefficiency to induce the internalization of mu opioid (MOP) receptors observed in numerous experimental models constitutes a paradigm of G-protein coupled receptor (GPCR) functional selectivity.
Alvarez-Curto, Elisa +2 more
core +1 more source