Physicochemical and biological properties of novel amide-based steroidal inhibitors of NMDA receptors
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61388963%3A_____%2F17%3A00474432" target="_blank" >RIV/61388963:_____/17:00474432 - isvavai.cz</a>
Alternative codes found
RIV/67985823:_____/17:00474432 RIV/00216208:11120/17:43912357 RIV/00216208:11320/17:10359502
Result on the web
<a href="http://dx.doi.org/10.1016/j.steroids.2016.08.010" target="_blank" >http://dx.doi.org/10.1016/j.steroids.2016.08.010</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1016/j.steroids.2016.08.010" target="_blank" >10.1016/j.steroids.2016.08.010</a>
Alternative languages
Result language
angličtina
Original language name
Physicochemical and biological properties of novel amide-based steroidal inhibitors of NMDA receptors
Original language description
Herein, we report a new class of amide-based inhibitors (1-4) of N-methyl-o-aspartate receptors (NMDARs) that were prepared as analogues of pregnanolone sulfate (PAS) and pregnanolone glutamate (PAG) - the steroidal neuroprotective NMDAR inhibitors. A series of experiments were conducted to evaluate their physicochemical and biological properties: (i) the inhibitory effect of compounds 3 and 4 on NMDARs was significantly improved (IC50 = 1.0 and 1.4 mu M respectively) as compared with endogenous inhibitor - pregnanolone sulfate (IC50 = 24.6 mu M) and pregnanolone glutamate (IC50 = 51.7 mu M), (ii) physicochemical properties (logP and logD) were calculated, (iii) Caco-2 assay revealed that the permeability properties of compounds 2 and 4 are comparable with pregnanolone glutamate, (iv) compounds 1-4 have minimal or no adverse hepatic effect, (v) compounds 1-4 cross blood-brain-barrier.
Czech name
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Czech description
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Classification
Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
10401 - Organic chemistry
Result continuities
Project
Result was created during the realization of more than one project. More information in the Projects tab.
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)
Others
Publication year
2017
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Steroids
ISSN
0039-128X
e-ISSN
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Volume of the periodical
117
Issue of the periodical within the volume
Jan
Country of publishing house
US - UNITED STATES
Number of pages
10
Pages from-to
52-61
UT code for WoS article
000392566800009
EID of the result in the Scopus database
2-s2.0-84994181912