Cholinergic properties of new 7-methoxytacrine-donepezil derivatives

Kód výsledku v 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>

Nalezeny alternativní kódy

RIV/67985823:_____/15:00448318 RIV/60162694:G44__/15:43875369 RIV/00023752:_____/15:43914720 RIV/62690094:18450/15:50003669 a 2 dalších

Výsledek na webu

<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>

Jazyk výsledku

angličtina

Název v původním jazyce

Cholinergic properties of new 7-methoxytacrine-donepezil derivatives

Popis výsledku v původním jazyce

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,

Název v anglickém jazyce

Cholinergic properties of new 7-methoxytacrine-donepezil derivatives

Popis výsledku anglicky

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,

Druh

J_x - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)

CEP obor

FR - Farmakologie a lékárnická chemie

OECD FORD obor

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Projekt

Výsledek vznikl pri realizaci vícero projektů. Více informací v záložce Projekty.

Návaznosti

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2015

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

General Physiology and Biophysics

ISSN

0231-5882

e-ISSN

—

Svazek periodika

34

Číslo periodika v rámci svazku

2

Stát vydavatele periodika

SK - Slovenská republika

Počet stran výsledku

12

Strana od-do

189-200

Kód UT WoS článku

000353181500009

EID výsledku v databázi Scopus

2-s2.0-84931084685