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Molecules 2014, 19(7), 8933-8948; doi:10.3390/molecules19078933

Flavonoids with M1 Muscarinic Acetylcholine Receptor Binding Activity

1
Department of Pharmacy, Faculty of Medicine, University of Malaya, 50603 Kuala Lumpur, Malaysia
2
Department of Chemistry, Faculty of Science, University of Malaya, 50603 Kuala Lumpur, Malaysia
3
School of Pharmacy and Health Sciences, International Medical University, Jalan Jalil Perkasa 19, Bukit Jalil, 57000 Kuala Lumpur, Malaysia
4
School of Pharmacy, University of Nottingham Malaysia Campus, Jalan Broga, 43500 Semenyih, Selangor Darul Ehsan, Malaysia
*
Authors to whom correspondence should be addressed.
Received: 27 February 2014 / Revised: 20 June 2014 / Accepted: 23 June 2014 / Published: 27 June 2014
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [4490 KB, uploaded 27 June 2014]   |  

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 (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. View Full-Text
Keywords: Alzheimer’s disease; muscarinic acetylcholine receptor; binding activity; flavonoids; molecular modelling Alzheimer’s disease; muscarinic acetylcholine receptor; binding activity; flavonoids; molecular modelling
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This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Swaminathan, M.; Chee, C.F.; Chin, S.P.; Buckle, M.J.C.; Rahman, N.A.; Doughty, S.W.; Chung, L.Y. Flavonoids with M1 Muscarinic Acetylcholine Receptor Binding Activity. Molecules 2014, 19, 8933-8948.

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