Flavonoids with M1 Muscarinic Acetylcholine Receptor Binding Activity

Overview

Journal Molecules

Publisher MDPI

Specialty Biology

Date 2014 Jul 1

PMID 24979399

Citations 8

Authors

Meyyammai Swaminathan

Chin Fei Chee

Sek Peng Chin

Michael J C Buckle

Noorsaadah Abd Rahman

Stephen W Doughty

Lip Yong Chung

Affiliations

Soon will be listed here.

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.

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