Cellular and behavioural effects of a new steroidal inhibitor of the N-methyl-D-aspartate receptor 3alfa5beta-pregnanolone glutamate

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60461373%3A22310%2F11%3A43891935" target="_blank" >RIV/60461373:22310/11:43891935 - isvavai.cz</a>

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 3alfa5beta-pregnanolone glutamate

Popis výsledku v původním jazyce

Preclin. 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 receptors inthe 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 NMDA receptor antagonist derived from naturally occurring neurosteroids. 20-oxo-5beta-pregnan-3alfa-yl-L-glutamyl-1-ester (3alfa5betaP-Glu) is a novel synthetic steroidal inhibitor of the NMDA receptor. Our results show that 3alfa5betaP-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 subs

Název v anglickém jazyce

Cellular and behavioural effects of a new steroidal inhibitor of the N-methyl-D-aspartate receptor 3alfa5beta-pregnanolone glutamate

Popis výsledku anglicky

Preclin. 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 receptors inthe 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 NMDA receptor antagonist derived from naturally occurring neurosteroids. 20-oxo-5beta-pregnan-3alfa-yl-L-glutamyl-1-ester (3alfa5betaP-Glu) is a novel synthetic steroidal inhibitor of the NMDA receptor. Our results show that 3alfa5betaP-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 subs

Druh

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

CEP obor

CC - Organická chemie

OECD FORD obor

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Projekt

—

Návaznosti

Z - Vyzkumny zamer (s odkazem do CEZ)

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

—

Svazek periodika

61

Číslo periodika v rámci svazku

1

Stát vydavatele periodika

BE - Belgické království

Počet stran výsledku

8

Strana od-do

61-68

Kód UT WoS článku

000292408200007

EID výsledku v databázi Scopus

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