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Muscarinic acetylcholine receptor-active compounds have potential for the treatment of Alzheimer’s disease. In this study, a series of natural and synthetic flavones and flavonols was assayed in vitro for their ability to inhibit radioligand binding at human cloned M1 muscarinic receptors. Several compounds were found to possess competitive binding affinity (Ki = 40–110 µM), comparable to that of acetylcholine (Ki = 59 µM). Despite the fact that these compounds lack a positively-charged ammonium group under physiological conditions, molecular modelling studies suggested that they bind to the orthosteric site of the receptor, mainly through non-polar interactions.
Binding Sites, Receptor, Muscarinic M1, Alzheimer’s disease; muscarinic acetylcholine receptor; binding activity; flavonoids; molecular modelling, muscarinic acetylcholine receptor, Organic chemistry, Muscarinic Agonists, Flavones, Article, Protein Structure, Secondary, molecular modelling, Protein Structure, Tertiary, Rats, Molecular Docking Simulation, QD241-441, flavonoids, Animals, Alzheimer’s disease, binding activity, Protein Binding
Binding Sites, Receptor, Muscarinic M1, Alzheimer’s disease; muscarinic acetylcholine receptor; binding activity; flavonoids; molecular modelling, muscarinic acetylcholine receptor, Organic chemistry, Muscarinic Agonists, Flavones, Article, Protein Structure, Secondary, molecular modelling, Protein Structure, Tertiary, Rats, Molecular Docking Simulation, QD241-441, flavonoids, Animals, Alzheimer’s disease, binding activity, Protein Binding
citations This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically). | 20 | |
popularity This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network. | Top 10% | |
influence This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically). | Top 10% | |
impulse This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network. | Average |