Flavonoids with M1 muscarinic acetylcholine receptor binding activity.
| Autor: | Swaminathan M; Department of Pharmacy, Faculty of Medicine, University of Malaya, 50603 Kuala Lumpur, Malaysia. oosh_mey@yahoo.com., Chee CF; Department of Chemistry, Faculty of Science, University of Malaya, 50603 Kuala Lumpur, Malaysia. cfchee@yahoo.com., Chin SP; Department of Pharmacy, Faculty of Medicine, University of Malaya, 50603 Kuala Lumpur, Malaysia. xueping.chin@gmail.com., Buckle MJ; Department of Pharmacy, Faculty of Medicine, University of Malaya, 50603 Kuala Lumpur, Malaysia. buckle@um.edu.my., Rahman NA; Department of Chemistry, Faculty of Science, University of Malaya, 50603 Kuala Lumpur, Malaysia. noorsaadah@um.edu.my., Doughty SW; School of Pharmacy, University of Nottingham Malaysia Campus, Jalan Broga, 43500 Semenyih, Selangor Darul Ehsan, Malaysia. stephen.doughty@nottingham.edu.my., Chung LY; Department of Pharmacy, Faculty of Medicine, University of Malaya, 50603 Kuala Lumpur, Malaysia. chungly@um.edu.my. |
|---|---|
| Jazyk: | angličtina |
| Zdroj: | Molecules (Basel, Switzerland) [Molecules] 2014 Jun 27; Vol. 19 (7), pp. 8933-48. Date of Electronic Publication: 2014 Jun 27. |
| DOI: | 10.3390/molecules19078933 |
| Abstrakt: | 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. |
| Databáze: | MEDLINE |
| Externí odkaz: |
|