Cholinergic properties of new 7-methoxytacrine-donepezil derivatives
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11310%2F15%3A10294600" target="_blank" >RIV/00216208:11310/15:10294600 - isvavai.cz</a>
Alternative codes found
RIV/67985823:_____/15:00448318 RIV/60162694:G44__/15:43875369 RIV/00023752:_____/15:43914720 RIV/62690094:18450/15:50003669 and 2 more
Result on the web
<a href="http://dx.doi.org/10.4149/gpb_2014036" target="_blank" >http://dx.doi.org/10.4149/gpb_2014036</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.4149/gpb_2014036" target="_blank" >10.4149/gpb_2014036</a>
Alternative languages
Result language
angličtina
Original language name
Cholinergic properties of new 7-methoxytacrine-donepezil derivatives
Original language description
Organophosphorus nerve agents inhibit acetylcholinesterase (AChE) which causes the breakdown of the transmitter acetylcholine (ACh) in the synaptic cleft. Overstimulation of cholinergic receptors (muscarinic and nicotinic) by excessive amounts of ACh causes several health problems and may even cause death. Reversible AChE inhibitors play an important role in prophylaxis against nerve agents. The presented study investigated whether 7-methoxytacrine (7-MEOTA) and 7-MEOTA-donepezil derivatives can act ascentral and peripheral reversible AChE inhibitors and simultaneously antagonize muscarinic and nicotinic receptors. The possible mechanism of action was studied on cell cultures (patch clamp technique, calcium mobilization assay) and on isolated smooth muscle tissue (contraction study). Furthermore, the kinetics of the compounds was also examined. CNS availability was predicted by determining the passive blood-brain barrier penetration estimated via a modified PAMPA assay. In conclusion,
Czech name
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Czech description
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Classification
Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
FR - Pharmacology and apothecary chemistry
OECD FORD branch
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Result continuities
Project
Result was created during the realization of more than one project. More information in the Projects tab.
Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Others
Publication year
2015
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
General Physiology and Biophysics
ISSN
0231-5882
e-ISSN
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Volume of the periodical
34
Issue of the periodical within the volume
2
Country of publishing house
SK - SLOVAKIA
Number of pages
12
Pages from-to
189-200
UT code for WoS article
000353181500009
EID of the result in the Scopus database
2-s2.0-84931084685