A resurrection of 7-MEOTA: a comparison with tacrine
Language English Country United Arab Emirates Media print
Document type Comparative Study, Journal Article, Research Support, Non-U.S. Gov't
PubMed
24093535
DOI
10.2174/1567205011310080011
PII: CAR-56335
Knihovny.cz E-resources
- MeSH
- Cholinesterase Inhibitors pharmacology MeSH
- Rats MeSH
- Oxidative Stress drug effects MeSH
- Rats, Wistar MeSH
- Tacrine analogs & derivatives pharmacology MeSH
- Animals MeSH
- Check Tag
- Rats MeSH
- Male MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Comparative Study MeSH
- Names of Substances
- 7-methoxytacrine MeSH Browser
- Cholinesterase Inhibitors MeSH
- Tacrine MeSH
Alzheimer´s disease (AD) is a progressive neurodegenerative dementia which currently represents one of the biggest threats for the human kind. The cure is still unknown and various hypotheses (cholinergic, amyloidal, oxidative, vascular etc.) are investigated in order to understand the pathophysiology of the disease and on this basis find an effective treatment. Tacrine, the first approved drug for the AD disease treatment, has been reported to be a multitargeted drug, however it was withdrawn from the market particularly due to its hepatotoxicity. Its derivative 7-methoxytacrine (7- MEOTA) probably due to the different metabolization does not exert this side effect. The aim of our study was to compare these two cholinesterase inhibitors from various, mainly cholinergic, points of view relevant for a potential AD drug. We found that 7-MEOTA does not fall behind its more well-known parent compound - tacrine. Furthermore, we found, that 7-MEOTA exerts better properties in most of the tests related to a possible AD treatment. Only the pharmacokinetics and a higher acetylcholinesterase and butyrylcholinesterase inhibitory potency would slightly give advantages to tacrine over 7-MEOTA, but concerning its lower toxicity, better antioxidant properties, interaction with muscarinic and nicotinic receptors and "safer" metabolization provide strong evidence for reconsider 7-MEOTA and its derivatives as candidate molecules for the treatment of AD.
References provided by Crossref.org
Sustainable Drug Discovery of Multi-Target-Directed Ligands for Alzheimer's Disease
In vitro investigating of anticancer activity of new 7-MEOTA-tacrine heterodimers
Technological Solutions for Older People with Alzheimer's Disease: Review
Development of 2-Methoxyhuprine as Novel Lead for Alzheimer's Disease Therapy
Alzheimer's disease and language impairments: social intervention and medical treatment