Flavonoids with M1 Muscarinic Acetylcholine Receptor Binding Activity
| Autor: | Stephen W. Doughty, Meyyammai Swaminathan, Noorsaadah Abd Rahman, Michael J. C. Buckle, Chin Fei Chee, Lip Yong Chung, Sek Peng Chin |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2014 |
| Předmět: |
Pharmaceutical Science
muscarinic acetylcholine receptor Muscarinic Agonists Pharmacology Flavones Article Protein Structure Secondary Analytical Chemistry lcsh:QD241-441 lcsh:Organic chemistry Drug Discovery Muscarinic acetylcholine receptor M5 Muscarinic acetylcholine receptor medicine Animals Physical and Theoretical Chemistry Binding site Receptor chemistry.chemical_classification Binding Sites Receptor Muscarinic M1 Organic Chemistry Alzheimer’s disease binding activity flavonoids molecular modelling Muscarinic acetylcholine receptor M3 Muscarinic acetylcholine receptor M1 Protein Structure Tertiary Rats Molecular Docking Simulation chemistry Biochemistry Chemistry (miscellaneous) Molecular Medicine Acetylcholine Protein Binding medicine.drug |
| Zdroj: | Molecules, Vol 19, Iss 7, Pp 8933-8948 (2014) Molecules; Volume 19; Issue 7; Pages: 8933-8948 Molecules |
| ISSN: | 1420-3049 |
| Popis: | 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: | OpenAIRE |
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