Cellular and behavioural effects of a new steroidal inhibitor of the N-methyl-d-aspartate receptor 3?5?-pregnanolone glutamate

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11120%2F11%3A00003164" target="_blank" >RIV/00216208:11120/11:00003164 - isvavai.cz</a>

Nalezeny alternativní kódy

RIV/67985823:_____/11:00364480 RIV/61388963:_____/11:00364480 RIV/00023752:_____/11:00001189

Výsledek na webu

<a href="http://dx.doi.org/10.1016/j.neuropharm.2011.02.018" target="_blank" >http://dx.doi.org/10.1016/j.neuropharm.2011.02.018</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.neuropharm.2011.02.018" target="_blank" >10.1016/j.neuropharm.2011.02.018</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Cellular and behavioural effects of a new steroidal inhibitor of the N-methyl-d-aspartate receptor 3?5?-pregnanolone glutamate

Popis výsledku v původním jazyce

Preclinical studies have demonstrated a considerable role for N-methyl-d-aspartate (NMDA) receptors in excitotoxicity and the concurrent neuroprotective effect of NMDA receptor antagonists. Because NMDA receptors are one of the most widespread receptorsin the central nervous system, application of their antagonist often leads to serious side effects ranging from motor impairment to induction of schizophrenic-like psychosis. Therefore, we have initiated development and testing of a novel synthetic NMDAreceptor antagonist derived from naturally occurring neurosteroids. 20-oxo-5?-pregnan-3?-yl-l-glutamyl-1-ester (3?5?P-Glu) is a novel synthetic steroidal inhibitor of the NMDA receptor. Our results show that 3?5?P-Glu preferentially inhibits tonically activated NMDA receptors, is able to cross the blood brain barrier, does not induce psychotomimetic symptoms (such as hyperlocomotion and sensorimotor gating deficit) and reduced an excitotoxic damage of brain tissue and subse

Název v anglickém jazyce

Cellular and behavioural effects of a new steroidal inhibitor of the N-methyl-d-aspartate receptor 3?5?-pregnanolone glutamate

Popis výsledku anglicky

Preclinical studies have demonstrated a considerable role for N-methyl-d-aspartate (NMDA) receptors in excitotoxicity and the concurrent neuroprotective effect of NMDA receptor antagonists. Because NMDA receptors are one of the most widespread receptorsin the central nervous system, application of their antagonist often leads to serious side effects ranging from motor impairment to induction of schizophrenic-like psychosis. Therefore, we have initiated development and testing of a novel synthetic NMDAreceptor antagonist derived from naturally occurring neurosteroids. 20-oxo-5?-pregnan-3?-yl-l-glutamyl-1-ester (3?5?P-Glu) is a novel synthetic steroidal inhibitor of the NMDA receptor. Our results show that 3?5?P-Glu preferentially inhibits tonically activated NMDA receptors, is able to cross the blood brain barrier, does not induce psychotomimetic symptoms (such as hyperlocomotion and sensorimotor gating deficit) and reduced an excitotoxic damage of brain tissue and subse

Druh

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

CEP obor

FH - Neurologie, neurochirurgie, neurovědy

OECD FORD obor

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Projekt

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

Návaznosti

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Rok uplatnění

2011

Kód důvěrnosti údajů

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

Název periodika

Neuropharmacology

ISSN

0028-3908

e-ISSN

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Svazek periodika

6

Číslo periodika v rámci svazku

1

Stát vydavatele periodika

GB - Spojené království Velké Británie a Severního Irska

Počet stran výsledku

8

Strana od-do

61-68

Kód UT WoS článku

000292408200007

EID výsledku v databázi Scopus

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