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Title: Flavonoids with M1 muscarinic acetylcholine receptor binding activity
Authors: Swaminathan, M. 
Chee, C.F. 
Chin, S.P. 
Buckle, M.J.C. 
Rahman, N.A. 
Doughty, S.W. 
Chung, L.Y. 
Keywords: Alzheimer's disease
Binding activity
Issue Date: 2014
Journal: Molecules Volume 19, Issue 7, July 2014, Pages 8933-8948 
Abstract: 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 (K i = 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.
DOI: 10.3390/molecules19078933
Appears in Collections:COE Scholarly Publication

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